Month: November 2022

Clinicopathological and prognostic value of necroptosis-associated lncRNA model in patients with kidney renal clear cell carcinoma was written by Gu, Jun;He, Zexi;Huang, Yinglong;Luan, Ting;Chen, Zhenjie;Wang, Jiansong;Ding, Mingxia. And the article was included in Disease Markers in 2022.Reference of 16506-27-7 The following contents are mentioned in the article:

Necroptosis, a recently identified type of programmed necrotic cell death, is closely related to the tumorigenesis and development of cancer. However, it remains unclear whether necroptosis-associated long noncoding RNAs (lncRNAs) can be used to predict the prognosis of kidney renal clear cell carcinoma (KIRC). This work was designed to probe the possible prognostic worth of necroptosis-associated lncRNAs along with their impact on the tumor microenvironment (TME) in KIRC. The Cancer Genome Atlas (TCGA) database was used to extract KIRC gene expression and clinicopathol. data. Pearson correlation anal. was used to evaluate necroptosis-associated lncRNAs against 159 known necroptosis-associated genes. To define mol. subtypes, researchers used univariate Cox regression anal. and consensus clustering, as well as clin. significance, TME, and tumor immune cells in each mol. subtype. We develop the necroptosis-associated lncRNA prognostic model using univariate Cox regression anal. and least absolute shrinkage and selection operator (LASSO) regression anal. Patients were divided into high- and low-risk groups according to prognostic model. Moreover, comprehensive analyses, including prognostic value, gene set enrichment anal. (GSEA), immune infiltration, and immune checkpoint gene expression, were performed between the two risk groups. Finally, anticancer drug sensitivity analyses were employed for assessing associations for necroptosis-associated lncRNA expression profile and anticancer drug chemosensitivity. Through univariate anal., sixty-nine necroptosis-associated lncRNAs were found to have a significant relationship with KIRC prognosis. Two mol. clusters were identified, and significant differences were found with respect to clinicopathol. features and prognosis. The segregation of patients into two risk groups was done by the constructed necroptosis-associated lncRNA model. The survival prognosis, clin. features, degree of immune cell infiltration, and expression of immune checkpoint genes of high-risk and low-risk groups were all shown to vary. Our study identified a model of necroptosis-associated lncRNA signature and revealed its prognostic role in KIRC. It is expected to provide a reference for the screening of KIRC prognostic markers and the evaluation of immune response. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7Reference of 16506-27-7).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Reference of 16506-27-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Effectiveness and tolerability of radiotherapy for patients with indolent non-Hodgkin’s lymphoma: a monocenter analysis was written by Hadi, I.;Schummer, A.;Dreyling, M.;Eze, C.;Bodensohn, R.;Roengvoraphoj, O.;Belka, C.;Li, M.. And the article was included in Scientific Reports in 2021.COA of Formula: C16H21Cl2N3O2 The following contents are mentioned in the article:

To analyze the effectiveness and toxicities of radiotherapy in indolent non-Hodgkin’s lymphoma (iNHL) patients treated in our institution. Patients with iNHL treated with radiotherapy between 1999 and 2016 were included. The primary endpoint was progression-free survival (PFS). Secondary endpoints were local control (LC), overall survival (OS) and toxicities. PFS, LC, and OS were analyzed using Kaplan-Meier method. Log-rank test was used to investigate the differences between subgroups. Cox proportional hazard model was used for univariate continuous anal. Seventy-five patients were identified in our institutional database between 1999 and 2016. Fifty-eight (77.3%) had stage I after Ann-Arbor and 17 patients (22.7%) had stage II. The median follow-up was 87 mo (95% CI 72-102 mo). Median single dose per fraction was 2.0 Gy (range 1.5-2 Gy) and median total dose was 30.6 Gy (range 16-45 Gy). Radiotherapy was performed in 2D (n = 10; 13.3%), 3D (n = 63; 84.0%) and VMAT (n = 2; 2.7%) techniques, resp. The median PFS was 14.0 years (95% CI 8.3-19.7 years). The estimated PFS after 5 and 10 years were 73.0% and 65.5% in Kaplan-Meier anal., resp. The 5- and 10-yr LC were 94.9% and 92.3%, resp. The 5- and 10-yr OS were 88.6% and 73.9%. In univariate analyses of PFS, younger patients (≤ 60 years old) had significantly superior PFS to those older than 60 years old (5-yr PFS 81.9% vs. 65.1%, p = 0.021). Dose escalation > 36.0 Gy had no prognostic influence in term of PFS (p = 0.425). Extranodal involvement, stage and histol. had no prognostic impact on PFS. Depending on the site of lymphomas, the most common acute side effects were: dermatitis CTCAE° I-II (8.0%), xerostomia CTC° I (8.0%), cataract CTC° I (12.0%) and dry eyes CTC° I-II (14.6%). No adverse event CTC° III was reported. Most acute side effects recovered at 3 to 6 mo after radiotherapy except for CTC° I cataract and xerostomia. Local Radiotherapy was highly effective for treatment of early stage iNHL with no serious side effects in our cohort. The most acute CTCAE° I-II side effects recovered 3 to 6 mo later. Technique advances seem to have further improved effectiveness and tolerability of radiotherapy. Local ethics committee of Ludwig-Maximilian-University (LMU) Munich approved this retrospective anal. on the May 7th, 2019 (Nr. 19-137). This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7COA of Formula: C16H21Cl2N3O2).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole is incorporated into many important biological compounds. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Histidine is present in many proteins and enzymes, e.g. by binding metal cofactors, as seen in hemoglobin.COA of Formula: C16H21Cl2N3O2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Post-transplantation cyclophosphamide uniquely restrains alloreactive CD4+ T-cell proliferation and differentiation after murine MHC-haploidentical hematopoietic cell transplantation was written by Hadjis, Ashley D.;Nunes, Natalia S.;Khan, Shanzay M.;Fletcher, Rochelle E.;de Paula Pohl, Alessandra;Venzon, David J.;Eckhaus, Michael A.;Kanakry, Christopher G.. And the article was included in Frontiers in Immunology in 2022.SDS of cas: 16506-27-7 The following contents are mentioned in the article:

Post-transplantation cyclophosphamide (PTCy) reduces the incidence and severity of graft-vs.-host disease (GVHD), thereby improving the safety and accessibility of allogeneic hematopoietic cell transplantation (HCT). We have shown that PTCy works by inducing functional impairment and suppression of alloreactive T cells. We also have identified that reduced proliferation of alloreactive CD4+ T cells at day +7 and preferential recovery of CD4+CD25+Foxp3+ regulatory T cells (Tregs) at day +21 are potential biomarkers associated with optimal PTCy dosing and timing in our B6C3F1!B6D2F1 MHC-haploidentical murine HCT model. To understand whether the effects of PTCy are unique and also to understand better the biol. of GVHD prevention by PTCy, here we tested the relative impact of cyclophosphamide compared with five other optimally dosed chemotherapeutics (methotrexate, bendamustine, paclitaxel, vincristine, and cytarabine) that vary in mechanisms of action and drug resistance. Only cyclophosphamide, methotrexate, and cytarabine were effective in preventing fatal GVHD, but cyclophosphamide was superior in ameliorating both clin. and histopathol. GVHD. Flow cytometric analyses of blood and spleens revealed that these three chemotherapeutics were distinct in constraining conventional T-cell numerical recovery and facilitating preferential Treg recovery at day +21. However, cyclophosphamide was unique in consistently reducing proliferation and expression of the activation marker CD25 by alloreactive CD4+Foxp3- conventional T cells at day +7. Furthermore, cyclophosphamide restrained the differentiation of alloreactive CD4+Foxp3- conventional T cells at both days +7 and +21, whereas methotrexate and cytarabine only restrained differentiation at day +7. No chemotherapeutic selectively eliminated alloreactive T cells. These data suggest that constrained alloreactive CD4+Foxp3- conventional T-cell numerical recovery and associated preferential CD4+CD25+Foxp3+ Treg reconstitution at day +21 may be potential biomarkers of effective GVHD prevention. Addnl., these results reveal that PTCy uniquely restrains alloreactive CD4+Foxp3- conventional T-cell proliferation and differentiation, which may explain the superior effects of PTCy in preventing GVHD. Further study is needed to determine whether these findings also hold true in clin. HCT. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7SDS of cas: 16506-27-7).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole derivatives generally have good solubility in protic solvents. Simple imidazole derivatives, such as 1H-imidazole, 2-methyl-1H-imidazole, and 1,2-dimethylimidazole, have very high solubility in water. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.SDS of cas: 16506-27-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

COVID-19 and CAR T cells: a report on current challenges and future directions from the EPICOVIDEHA survey by EHA-IDWP was written by Busca, Alessandro;Salmanton-Garcia, Jon;Corradini, Paolo;Marchesi, Francesco;Cabirta, Alba;Di Blasi, Roberta;Dulery, Remy;Lamure, Sylvain;Farina, Francesca;Weinbergerova, Barbora;Batinic, Josip;Nordlander, Anna;Lopez-Garcia, Alberto;Drgona, Lubos;Espigado-Tocino, Ildefonso;Falces-Romero, Iker;Garcia-Sanz, Ramon;Garcia-Vidal, Carolina;Guidetti, Anna;Khanna, Nina;Kulasekararaj, Austin;Maertens, Johan;Hoenigl, Martin;Klimko, Nikolai;Koehler, Philipp;Pagliuca, Antonio;Passamonti, Francesco;Cornely, Oliver A.;Pagano, Livio. And the article was included in Blood Advances in 2022.Reference of 16506-27-7 The following contents are mentioned in the article:

The aim of this study was to describe the clin. outcomes of patients developing COVID-19 after treatment with CAR T cells. In this retrospective observational multicenter study, collected data on all consecutive adult patients who received CAR T-cell therapy with symptomatic COVID-19 between Jan. 2020 and Feb. 2021 across 18 European centers (Spain, n = 6; France, n = 3; Italy, n = 2; and Belgium, Croatia, Czechia, Slovakia, Sweden, Switzerland, and the United Kingdom, n = 1 each) participating in the survey promoted by the European Hematol. Association (EHA) Scientific Working Group on Infection in Hematol. (EPICOVI- DEHA survey), developed by the EHA Infectious Diseases Working Party (IDWP). Patients received CAR T cells for the treatment of large B-cell lymphoma (n 5 28), multiple myeloma (n 5 1), and acute lymphoblastic leukemia (n 5 1). CAR T cells were tisagenlecleucel (Kymriah) in 16 cases and axicabtagene (Yescarta) in 13 cases, and 1 patient with multiple myeloma was treated with CAR T cells targeting B-cell maturation antigen. Median time from CAR T-cell treatment to COVID-19 diagnosis was 169 days (IQR, 37-313; range, 1-635). Cellular and humoral immune reconstitution after CAR T cells showed that 90 days after infusion, median absolute neutrophil count and absolute lymphocyte count (ALC) were 1700/mm3 and 435/mm3 resp., whereas at the time of COVID-19 diagnosis, median absolute neutrophil count and ALC were 925/mm3 and 370/mm3 resp. In total, 13 patients (43.3%) required admission to ICU after COVID-19, and 9 of them (66.7%) required mech. ventilation. Patients received treatment for COVID-19 according to local policy; 15 patients were treated with convalescent plasma alone (n = 3) or convalescent plasma combined with remdesivir with or without steroids (n = 8), remdesivir with lopinavir/ritonavir and steroids (n = 1), and tocilizumab and steroids (n = 3); 5 patients were treated with steroids alone (n = 4) or steroids combined with remdesivir and tocilizumab (n = 1); 1 patient was treated with azithromycin; and patient was treated with remdesivir alone. Severe (grade > 3) CRS after CAR T cells was observed in 1 patient only, and in total, 8 (53.3%) of 15 patients who developed CRS after CAR T-cell infusion required treatment with tocilizumab with or without steroids. Therapeutic strategies will need to be developed to ensure that CAR T-cell therapy can be delivered safely and successfully while COVID-19 remains endemic. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7Reference of 16506-27-7).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Reference of 16506-27-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Cationic Ir(III) Complexes Featuring Phenylimidazole-type Cyclometalated Ligands: Fluorine-Free Blue Phosphorescent Emitters for Light-Emitting Devices was written by Song, Yongjun;Yu, Renyou;Chen, Mengzhen;He, Lei. And the article was included in Inorganic Chemistry in 2021.HPLC of Formula: 914306-50-6 The following contents are mentioned in the article:

The development of blue emissive cationic Ir(III) complexes with no F substitutions but with sufficient blue-color purity and high phosphorescence efficiency has remained challenging. Here, F-free cyan to deep-blue emissive cationic Ir(III) complexes with phenylimidazole type cyclometalated ligands (CN̂) are reported, which are [Ir(dphim)₂(dmapzpy)]PF₆ (1), [Ir(ipr-dphim)₂(dmapzpy)]PF₆ (2), [Ir(ipr-dphim)₂(bipz)]PF₆ (3), and [Ir(ipr-dphim)₂(bicb)]PF₆ (4). 1,2-diphenyl-1H-imidazole (dphim) and 1-(2,6-diisopropylphenyl)-2-phenyl-1H-imidazole (ipr-dphim) are the phenylimidazole type CN̂ ligands, and 4-dimethylamino-2-(1H-pyrazol-1-yl)pyridine (dmapzpy), di(1H-pyrazol-1-yl)methane (bipz), and 3,3′-methylenebis(1-Me-1H-imidazol-3-ium-2-ide) (bicb) are the neutral ancillary ligands (AÂ). In both solution and diluted films, 1 shows cyan emission with the emission maximum at ∼472 and 495 nm, and 2–4 provide deep-blue emission with the emission maximum at ∼460 and 480 nm. While the complexes exhibit low to moderate phosphorescent efficiencies (0.05-0.35) in degassed MeCN solution, they exhibit high phosphorescent efficiencies (≤0.82) in diluted films. Theor. calculations revealed that the mixed ³π-π^* (CN̂-centered)/³MLCT (Ir → CN̂) states are responsible for the emission afforded by 1–4, which undergo nonradiative deactivations induced by different types of metal-centered states. Organic light-emitting diodes (OLEDs) with 1–4 as phosphorescent dopants are fabricated by solution-process, which afford blue-green to blue emission with the emission maximum at ∼460 and 490 nm for the blue devices and a high current-efficiency at 28.1 cd A^-1 for the blue-green device. Solid-state light-emitting electrochem. cells (LECs) are fabricated with 1–2 as phosphorescent dopants, which provide green-blue to blue emission with high luminance (up to 840 cd m^-2) and current-efficiency (≤16.8 cd A^-1) under a constant-current driving. By using phenylimidazole type CN̂ ligands and optimized AÂ ligands, blue emissive cationic Ir(III) complexes with no F substitutions but with sufficient blue-color purity and high phosphorescence efficiency can be developed. This study involved multiple reactions and reactants, such as 1-(2,6-Diisopropylphenyl)-2-phenyl-1H-imidazole (cas: 914306-50-6HPLC of Formula: 914306-50-6).

1-(2,6-Diisopropylphenyl)-2-phenyl-1H-imidazole (cas: 914306-50-6) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.HPLC of Formula: 914306-50-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Bioequivalence of a Newly Developed Dabigatran Etexilate Tablet Versus the Commercial Capsule and Impact of Rabeprazole-Induced Elevated Gastric pH on Exposure in Healthy Subjects was written by Harada, Akiko;Ikushima, Ippei;Haranaka, Miwa;Yanagihara, Aki;Nakayama, Daisuke. And the article was included in American Journal of Cardiovascular Drugs in 2020.Formula: C18H20N3NaO3S The following contents are mentioned in the article:

Background and Objective: Dabigatran etexilate (DE) is an anticoagulant with proven efficacy and tolerability for stroke prevention in patients with non-valvular atrial fibrillation. For the com. capsule, a complex formulation is used to maintain the acidic microenvironment required for maximal absorption. Consequently, its efficacy and safety are similar with or without concomitant intake of proton-pump inhibitors (PPIs). A simplified DE tablet formulation was developed and tested in two studies. One investigated bioequivalence (BE) of the novel DE tablet vs. the com. DE capsule. The other investigated DE bioavailability (BA) under pretreatment with the PPI rabeprazole and assessed the effect of elevated pH on exposure to dabigatran. Methods: BE of the novel DE tablet vs. the DE capsule was assessed in a randomized two-treatment, four-period, two-sequence crossover study (NCT03070171). The effect of rabeprazole on the BA of the DE tablet was assessed in an open-label, single-arm study (NCT03143166). Both studies were conducted at sites in Japan. Participants were healthy male volunteers, aged ≥ 20-40 years. In the BE study, participants received the DE tablet or capsule (single oral dose, 110 mg); primary endpoints were area under the concentration-time curve from baseline to the last quantifiable data point (AUC_0-tz) and maximum plasma concentration (C_max) of unconjugated dabigatran. In the relative BA study, participants received the DE tablet (single oral dose, 110 mg) with or without rabeprazole pretreatment (once daily for 5 days, 20 mg); primary endpoints were AUC_0-tz and C_max of total dabigatran. Results: In total, 160 participants were randomized in the BE study; 36 participants were enrolled in the BA study. The 90% confidence intervals of geometric mean (gMean) ratios for AUC_0-tz (101.4-116.0%) and C_max (101.8-116.6%) of unconjugated dabigatran were within pre-defined acceptance criteria for BE. In the relative BA study, the gMeans of AUC_0-tz (667 to 192 ng h/mL) and C_max (83.1 to 21.8 ng/mL) were decreased by approx. 70% when the tablet was administered under rabeprazole pretreatment. The reduction in BA was observed at a mean gastric pH of 5.3. Treatment was well tolerated; no deaths, serious adverse events (AEs) or significant AEs were reported in either study. Conclusion: The DE tablet demonstrated BE to the capsule; however, at high gastric pH, BA of the tablet was reduced by approx. 70%, which may lead to reduced efficacy. Data indicate the importance of examining not only BE under standard conditions, but relative BA at elevated gastric pH. Such investigations may avoid the reduced BA at elevated pH that is quite common in the target population (the elderly and/or patients treated with gastric-acid modifying co-medications), and therefore reduce treatment failure with DE. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Formula: C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.Formula: C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazoles. IX. A new preparation of N-alkylated imidazole compounds was written by Weidenhagen, Rudulf;Train, Gert;Wegner, Hans;Nordstrom, Ludwig. And the article was included in Berichte der Deutschen Chemischen Gesellschaft [Abteilung] B: Abhandlungen in 1942.Name: 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine The following contents are mentioned in the article:

A solution of 2 g. Cu(OAc)₂, 2 cc. 40% HCHO and 30 cc. H₂O at 0° is treated with 1 g. ο-H₂NC₆H₄NHMe.2HCl in 15 cc. 50% alc. at 0°; the CuCl salt precipitates immediately and the reaction is completed by heating 10 min. at 75°; decomposition with H₂S in dilute HCl gives the HCl salt, which is liberated by K₂CO₃; the yield of 1-methylbenzimidazole (I) is 67%; AcH gives 83% of the 2-Me derivative of I; EtCHO yields the 2-Et derivative, very hygroscopic, m. 61.5-2.5° (containing 0.79 mol. H₂O), m. 54.5-5.5° (anhydrous); picrate, m. 235-6°; iso-PrCHO gives 84% of the 2-iso-Pr derivative, b_0.3 116-18° (picrate, yellow, m. 225-6°); BzH gives 87.5% of the 2-Ph derivative; p-MeOC₆H₄CHO yields 77.5% of the 2-(p-methoxyphenyl) derivative, m. 118°; 2-(p-nitrophenyl) derivative, yellow, m. 213-14°, 88%; 2-(2-furyl) derivative, with 0.5 mol. H₂O, m. 78° (anhydrous, m. 56°), 85%. ο-O₂NC₆H₄NHEt with SnCl₂ in HCl gives 69% of N-ethyl-ο-phenylenediamine (II), m. 185-7° (decomposition). II, HCHO and Cu(OAc)₂ give 71% of 1-ethylbenzimidazole (III); AcH yields 90% of the 2-Me derivative of III, b_0.3 110-12° (picrate, m. 236-7°); EtCHO gives 74% of the 2-Et derivative of III, b_0.2 106.5-7.5° (HCl salt, m. 168.5-9.5°; picrate, m. 207°); BzH yields 82% of the 2-Ph derivative of III; 2-(p-methoxyphenyl) derivative, m. 106-6.5°, 90%; 2-(m-nitrophenyl) derivative, m. 117.5-18°, 46%. ο-ClC₆H₄NO₂ and PrNH₂ in EtOH, heated 7 hrs., give 97% of N-propyl-ο-nitroaniline, red oil; reduction yields 57% of N-propyl-ο-phenylenediamine-2-HCl (IV), m. 172-3° (decomposition). IV, HCHO and Cu(OAc)₂ give 62% of 1-propylbenzimidazole (V), analyzed as the picrate, m. 180-1°; IV and AcH give 92% of the 2-Me derivative of V, hygroscopic oil, b_0.2 111-12° (picrate, m. 218-19°); 2-Et derivative, 85%; picrate, m. 212-12.5°; 2-(p-methoxyphenyl) derivative, m. 67.5-8°. 3-Amino-4-(methylamino)pyridine (VI), m. 169°, results in 95% yield on reduction of the 3-NO₂ compound with Fe in AcOH (picrate, m. 184°; HCl salt, m. 221°). VI (1.8 g.), 1 cc. AcH and 6 g. Cu(OAc)₂ in 50 cc. 50% EtOH, heated 3 hrs. at 150°, give 50% of 1′,2′-dimethylimidazolo-4′,5′,3,4-pyridine (VII), m. 174° (picrate, m. 204-5°); EtCHO gives 48% of the 2′-Et analog of VII, with 1.5 mols. H₂O, m. 76°; 2′-Pr analog, with 1.5 mols. H₂O, m. 64°, 59%; 2′-hexyl analog, a hygroscopic oil, analyzed as the dioxalate, m. 140°, 47%; 2′-Ph analog, m. 149°, 49% (hydrated, m. 79-80°); 2′-(2-furyl) analog, m. 173°, 57%. 3-Amino-4-(ethylamino)pyridine, AcH and Cu(OAc)₂ in EtOH, heated 4.5 hrs. at 150°, give 1′-ethyl-2′-methylimidazolo-4′,5′,3,4-pyridine, m. 84°; with 1 mol. of H₂O, m. 40°; picrate, m. 191°; 2′-Et analog, hygroscopic oil; with 2 mols. H₂O, m. 52°, 54%; 2′-Pr analog, very hygroscopic oil, 39%; with 2 mols. H₂O, m. 68°; 2′-(p-methoxyphenyl) analog, m. 142°, 71%; 2′-(2-furyl) analog, pale yellow, m. 125°, 68%. 3-Nitro-4-(propylamino)pyridine, in nearly theoretical yield by boiling 3-nitro-4-methoxypyridine with PrNH₂ in EtOH; 3-NH₂ derivative, with 1 mol. H₂O, m. 93°, 78%. 1′-Propyl-2′-methylimidazolo-4′,5′,3,4-pyridine, analyzed as the picrate, yellow, m. 156.5-7.5°; 1′-Bu analog, with 2 mols H₂O, m. 47°, 58%. This study involved multiple reactions and reactants, such as 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine (cas: 52538-09-7Name: 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine).

2,3-Dimethyl-3H-imidazo[4,5-c]pyridine (cas: 52538-09-7) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Name: 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Graft-versus-Host Disease Prophylaxis with Post-Transplantation Bendamustine in Patients with Refractory Acute Leukemia: A Dose-Ranging Study was written by Moiseev, Ivan;Bondarenko, Sergey;Morozova, Elena;Vlasova, Yulia;Dotsenko, Anna;Epifanovskaya, Olga;Babenko, Elena;Botina, Anna;Baykov, Vadim;Surkova, Elena;Lapin, Sergey;Beynarovich, Anastasiya;Borzenkova, Evgeniya;Golosgchapov, Oleg;Kanunnikov, Mikhail;Kudyasheva, Olga;Ovechkina, Varvara;Pirogova, Olga;Porunova, Valentina;Rudakova, Tatyana;Smikova, Olesya;Smirnova, Anna;Afansyev, Boris. And the article was included in Transplantation and Cellular Therapy in 2021.HPLC of Formula: 16506-27-7 The following contents are mentioned in the article:

The prognosis of acute leukemia refractory to induction chemotherapy or immunotherapy is dismal. Salvage allogeneic hematopoietic stem cell transplantation (HSCT) is widely used option for these patients, but only 10% to 15% of patients are cured by the procedure. Preclin. studies indicate that substitution of post-transplantation cyclophosphamide with bendamustine (PTB) in a prophylaxis regimen may be associated with an augmented graft-vs.-leukemia (GVL) reaction. The aim of this study was to establish the optimal dose of PTB and evaluate the antileukemic effect of HSCT with this type of graft-vs.-host disease (GVHD) prophylaxis. In the prospective trial (NCT02799147), PTB was administered in doses of 140, 100, and 70 mg/m2 on days +3 and +4. Myeloablative conditioning with fludarabine and oral busulfan was provided to all patients. The first 12 patients received single-agent PTB, and subsequent patients received combination therapy with tacrolimus and mycophenolate mofetil (MMF). Inclusion criteria were acute myelogenous leukemia (AML) or acute lymphoblastic leukemia (ALL) refractory to at least one induction course of chemotherapy or target therapy and ≥5% clonal blasts in the bone marrow. The study cohort comprised 22 patients with AML and 5 with ALL. Seven patients were enrolled in the 140 mg/m2 group (due to a stopping rule), and 10 each were enrolled in the 100 mg/m2 and 70 mg/m2 groups. Primary refractory disease was documented in 41% of the patients, and secondary refractory was documented in 59%. The median blast count in the bone marrow at the start of the conditioning was 18% (range, 6% to 97%). Transplantation was performed with a matched sibling donor in 5 patients, a matched or mismatched unrelated donor in 15, and a haploidentical donor in 7. Engraftment was documented in 93% of the patients, including 89% with complete remission and 63% without measurable residual disease. After PTB prophylaxis, we observed an unusual complication, a cytokine release syndrome (CRS), in 70% of the patients, including grade 3 to 5 CRS in 44%. The most frequent clin. symptoms included high fever in 67% of patients, abnormal liver function tests in 67%, pancreatitis in 63%, skin vasculitis in 56%, enterocolitis in 48%, inflammation of oral mucosa in 37%, disseminated intravascular coagulation in 37%, and central nervous system toxicity in 26%. The development of CRS was associated with use of an HLA-mismatched donor (75% vs. 20%; P = .0043). Classic acute GVHD was documented in 44% of the patients. Grade II-IV acute GVHD was associated with grade 3 to 5 CRS (67% vs. 25%; P = .031). Moderate and severe chronic GVHD in the 100-day survivors were more often observed after single-agent PTB than after the combination immunosuppression (100% vs. 18%; P = .002). A relatively low relapse rate was observed for this patient population. Three-year overall survival was 28% (95% confidence interval [CI], 13% to 46%), and event-free survival was 29% (95% CI, 13% to 46%). Nonrelapse mortality was 46% (95% CI, 25% to 64%), and the cumulative incidence of relapse was 26% (95% CI, 11% to 44%). No relapses were documented after day +100. There were no statistically significant differences among the dose groups (P = .3481); however, survival was higher in the 100 mg/kg group. Survival was higher in patients with AML compared with those with ALL (35% vs. 0%; P = .0157). PTB represents a promising option to augment the GVL effect in refractory AML; however, the high CRS-associated mortality necessitates addnl. studies to reduce the risk of this complication. Thus, routine clin. application of PTB cannot be currently recommended. Combination immunosuppression with tacrolimus and MMF partially ameliorates these complications, at least in the setting of HLA-matched allografts. Biol. mechanisms of CRS and GVL after PTB require further elucidation. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7HPLC of Formula: 16506-27-7).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.HPLC of Formula: 16506-27-7

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Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem