Category: imidazoles-derivatives

On May 31, 2020, Feng, Jingxian; Xu, Minjun; Wang, Jiahao; Zhou, Songlei; Liu, Yipu; Liu, Shanshan; Huang, Yukun; Chen, Yu; Chen, Liang; Song, Qingxiang; Gong, Jingru; Lu, Huiping; Gao, Xiaoling; Chen, Jun published an article.Product Details of 5036-48-6 The title of the article was Sequential delivery of nanoformulated ä¼?mangostin and triptolide overcomes permeation obstacles and improves therapeutic effects in pancreatic cancer. And the article contained the following:

Pancreatic ductal adenocarcinoma (PDAC) is a devastating disease exhibiting the poorest prognosis among solid tumors. The efficacy of conventional therapies has been hindered largely due to the insufficient chemotherapeutic delivery to the dense desmoplastic tumor stroma, and the extremely high or toxic dose needed for chemotherapy. Traditional Chinese Medicine (TCM) contains effective components that can effectively regulate tumor microenvironment and kill tumor cells, providing promising alternatives to PDAC chemotherapy. In this study, two active drug monomers of TCM were screened out and a sequentially targeting delivery regimen was developed to realize the optimized combinational therapy. Transforming growth factor-å°?(TGF-å°? plays an indispensable role in promoting cancer-associated fibroblasts (CAFs) activation and proliferation, and CAFs have caused major phys. barriers for chemotherapeutic drug delivery. Herein, CAFs-targeting biodegradable polymer nanoparticle (CRE-NP(ä¼?M)) coated with CREKA peptide and loaded with TCM ä¼?mangostin (ä¼?M) was developed to modulate tumor microenvironment by interfering of TGF-å°?Smad signaling pathway. Low pH-triggered micelle modified with CRPPR peptide and loaded with another TCM triptolide was constructed to increase the therapeutic effect of triptolide at the tumor sites and reduced its damage to main organs. As expected, CRE-NP(ä¼?M) effectively inactived CAFs, reduced extracellular matrix production, promoted tumor vascular normalization and enhanced blood perfusion at the tumor site. The sequentially targeting drug delivery regimen, CRP-MC(Trip) following CRE-NP(ä¼?M) pretreatment, exhibited strong tumor growth inhibition effect in the orthotopic tumor model. Hence, sequentially targeting delivery of nanoformulated TCM offers an efficient approach to overcome the permeation obstacles and improve the effect of chemotherapy on PDAC, and provides a novel option to treat desmoplastic tumors. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Product Details of 5036-48-6

The Article related to mangostin triptolide pancreatic cancer drug nanoformulation, acid-triggered micelles, pancreatic cancer, tgf-å°? traditional chinese medicine, triptolide, ä¼?mangostin, Placeholder for records without volume info and other aspects.Product Details of 5036-48-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On November 30, 2021, Liu, Zhen-zhen; Liu, Xiao-ning; Fan, Rui-cheng; Jia, Yu-ping; Zhang, Qing-ke; Gao, Xin-qing; Wang, Yu-qing; Yang, Meng-qing; Ji, Li-zhen; Zhou, Yong-qing; Li, Hong-li; Li, Ping; Tang, Bo published an article.Recommanded Product: 73590-85-9 The title of the article was Identification of pimavanserin tartrate as a potent Ca2+-calcineurin-NFAT pathway inhibitor for glioblastoma therapy. And the article contained the following:

Glioblastoma multiforme (GBM) is the most common and malignant type of primary brain tumor, and 95% of patients die within 2 years after diagnosis. In this study, aiming to overcome chemoresistance to the first-line drug temozolomide (TMZ), we carried out research to discover a novel alternative drug targeting the oncogenic NFAT signaling pathway for GBM therapy. To accelerate the drug鈥瞫 clin. application, we took advantage of a drug repurposing strategy to identify novel NFAT signaling pathway inhibitors. After screening a set of 93 FDA-approved drugs with simple structures, we identified pimavanserin tartrate (PIM), an effective 5-HT2A receptor inverse agonist used for the treatment of Parkinson鈥瞫 disease-associated psychiatric symptoms, as having the most potent inhibitory activity against the NFAT signaling pathway. Further study revealed that PIM suppressed STIM1 puncta formation to inhibit store-operated calcium entry (SOCE) and subsequent NFAT activity. In cellula, PIM significantly suppressed the proliferation, migration, division, and motility of U87 glioblastoma cells, induced G1/S phase arrest and promoted apoptosis. In vivo, the growth of s.c. and orthotopic glioblastoma xenografts was markedly suppressed by PIM. Unbiased omics studies revealed the novel mol. mechanism of PIM鈥瞫 antitumor activity, which included suppression of the ATR/CDK2/E2F axis, MYC, and AuroraA/B signaling. Interestingly, the genes upregulated by PIM were largely associated with cholesterol homeostasis, which may contribute to PIM鈥瞫 side effects and should be given more attention. Our study identified store-operated calcium channels as novel targets of PIM and was the first to systematically highlight the therapeutic potential of pimavanserin tartrate for glioblastoma. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Recommanded Product: 73590-85-9

The Article related to pimavanserin tartrate calcium calcineurin nfat inhibitor glioblastoma therapy, nfat signaling pathway, soce, drug repurposing, glioblastoma, pimavanserin tartrate, Placeholder for records without volume info and other aspects.Recommanded Product: 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Venkata Mallavadhani, Uppuluri; Vanga, Nagi Reddy; Balabhaskara Rao, Kancharana; Jain, Nishanth published an article in 2020, the title of the article was Synthesis and antiproliferative activity of novel (+)- usnic acid analogues.Name: N-(3-Aminopropyl)-imidazole And the article contains the following content:

Twenty one novel (+)- usnic acid-based analogs belonging to three classes such as enamines, imines, and pyrazoles were synthesized. All the synthesized compounds were characterized by their spectral data (1H NMR, 13C NMR, IR, and HRMS). The synthesized compounds were evaluated for their antiproliferative activity against a panel of four human cancer cell lines including HeLa (cervix), MDA-MB-231 (breast), A549 (lung), and MiaPaca (pancreas) by employing SRB cell proliferation assay. Screening results indicated that all synthesized compounds showed enhanced activity than the parent compound Most significantly, compounds and showed potent antiproliferative activity against all the cancer cell lines tested. Compounds and arrested the cell cycle in G2/M phase and induced apoptosis in HeLa cells. In view of significant antiproevaliferative activity, compounds and can be considered as lead mols. for further development. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Name: N-(3-Aminopropyl)-imidazole

The Article related to cervical lung breast pancreatic cancer antiproliferative usnic acid, (+)- usnic acid, antiproliferative activity, apoptosis, cell cycle arrest, enamine, pyrazole, Placeholder for records without volume info and other aspects.Name: N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 5, 2021, Qiu, Xiang; Wang, Shushu; Miao, Shanshan; Suo, Hongbo; Xu, Huajin; Hu, Yi published an article.Name: N-(3-Aminopropyl)-imidazole The title of the article was Co-immobilization of laccase and ABTS onto amino-functionalized ionic liquid-modified magnetic chitosan nanoparticles for pollutants removal. And the article contained the following:

This work aims to achieve the co-immobilization of laccase and 2,2-binamine-di-3-ethylbenzothiazolin-6-sulfonic acid (ABTS) to improve removal capability of the biocatalyst for pollutants while avoiding potential pollution caused by ABTS. The laccase was immobilized on magnetic chitosan nanoparticles modified with amino-functionalized ionic liquid containing ABTS (MACS-NIL) based on Cu ion chelation (MACS-NIL-Cu-lac). The carrier was characterized by Fourier transform IR spectroscopy, thermogravimetric anal., x-ray diffraction and etc., and ESR confirmed the mediator mol. ABTS on the carrier could also play the role of electron transmission. MACS-NIL-Cu-lac presented relatively high immobilization capacity, enhanced activity (1.7-fold that of free laccase), improved pH and temperature adaptability, and increased thermal and storage stability. The removal performance assay found that MACS-NIL-Cu-lac had a good removal efficiency with 100.0 % for 2,4-dichlorophenol in water at 25 掳C, even when the concentration reached 50 mg/L. Reusability study showed that after six catalytic runs, the removal efficiency of 2,4-dichlorophenol by MACS-NIL-Cu-lac could still reach 93.2 %. Addnl., MACS-NIL-Cu-lac exhibited higher catalytic efficiencies with 100.0 %, 70.5 % and 93.3 % for bisphenol A, indole, and anthracene, resp. The high catalytic performance in pure water system obtained by the novel biocatalyst co-immobilizing laccase and electron mediator ABTS showed greater practical application value. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Name: N-(3-Aminopropyl)-imidazole

The Article related to laccase abts immobilization magnetic chitosan nanoparticle pollutant removal, abts, ionic liquid, laccase, magnetic chitosan nanoparticles, pollutants removal, Placeholder for records without volume info and other aspects.Name: N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Li, Yin; Gu, Jie; Xu, Fengkai; Zhu, Qiaoliang; Chen, Yiwei; Ge, Di; Lu, Chunlai published an article in 2021, the title of the article was Molecular characterization, biological function, tumor microenvironment association and clinical significance of m6A regulators in lung adenocarcinoma.Recommanded Product: N-Methyl-7H-purin-6-amine And the article contains the following content:

N6-methyladenosine (m6A) modification can regulate a variety of biol. processes. However, the implications of m6A modification in lung adenocarcinoma (LUAD) remain largely unknown. Here, we systematically evaluated the m6A modification features in more than 2400 LUAD samples by analyzing the multi-omics features of 23 m6A regulators.We depicted the genetic variation features of m6A regulators, and found mutations of FTO and YTHDF3 were linked to worse overall survival. Many m6A regulators were aberrantly expressed in tumors, among which FTO, IGF2BP3, YTHDF1 and RBM15 showed consistent alteration features across 11 independent cohorts. Besides, the regulator-pathway interaction network demonstrated that m6A modification was associated with various biol. pathways, including immune-related pathways. The correlation between m6A regulators and tumor microenvironment was also assessed.We found that LRPPRC was neg. correlated with most tumor-infiltrating immune cells. On the other hand, we established a scoring tool named m6Sig, which was pos. correlated with PD-L1 expression and could ref lect both the tumor microenvironment characterization and prognosis of LUAD patients. Comparison of CNV between high and low m6Sig groups revealed differences on chromosome 7. Application of m6Sig on an anti-PD-L1 immunotherapy cohort confirmed that the high m6Sig group demonstrated therapeutic advantages and clin. benefits. Our study indicated that m6A modification is involved in many aspects of LUAD and contributes to tumor microenvironment formation. A better understanding of m6A modification will provide more insights into the mol. mechanisms of LUAD and facilitate developing more effective personalized treatment strategies. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Recommanded Product: N-Methyl-7H-purin-6-amine

The Article related to lung adenocarcinoma tumor microenvironment biol function, pd-l1 immunotherapy, lung adenocarcinoma, m6a, prognosis, tumor microenvironment, web application, Placeholder for records without volume info and other aspects.Recommanded Product: N-Methyl-7H-purin-6-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On December 31, 2021, Nguyen, Trinh Trung Duong; Trinh, Van Ngu; Le, Nguyen Quoc Khanh; Ou, Yu-Yen published an article.Application of 443-72-1 The title of the article was Using k-mer embeddings learned from a Skip-gram based neural network for building a cross-species DNA N6-methyladenine site prediction model. And the article contained the following:

Key message: This study used k-mer embeddings as effective feature to identify DNA N6-Methyladenine sites in plant genomes and obtained improved performance without substantial effort in feature extraction, combination and selection. Identification of DNA N6-methyladenine sites has been a very active topic of computational biol. due to the unavailability of suitable methods to identify them accurately, especially in plants. Substantial results were obtained with a great effort put in extracting, heuristic searching, or fusing a diverse types of features, not to mention a feature selection step. In this study, we regarded DNA sequences as textual information and employed natural language processing techniques to decipher hidden biol. meanings from those sequences. In other words, we considered DNA, the human life book, as a book corpus for training DNA language models. K-mer embeddings then were generated from these language models to be used in machine learning prediction models. Skip-gram neural networks were the base of the language models and ensemble tree-based algorithms were the machine learning algorithms for prediction models. We trained the prediction model on Rosaceae genome dataset and performed a comprehensive test on 3 plant genome datasets. Our proposed method shows promising performance with AUC performance approaching an ideal value on Rosaceae dataset (0.99), a high score on Rice dataset (0.95) and improved performance on Rice dataset while enjoying an elegant, yet efficient feature extraction process. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Application of 443-72-1

The Article related to neural network dna n6 methyladenine, dna n6-methyladenine site prediction, ensemble tree-based algorithms, natural language processing, k-mer embeddings, Placeholder for records without volume info and other aspects.Application of 443-72-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 3, 2021, Zeng, Juan; Zhang, Heying; Tan, Yonggang; Wang, Zhe; Li, Yunwei; Yang, Xianghong published an article.Synthetic Route of 443-72-1 The title of the article was m6A demethylase FTO suppresses pancreatic cancer tumorigenesis by demethylating PJA2 and inhibiting Wnt signaling. And the article contained the following:

Pancreatic cancer is the deadliest malignancy of the digestive system and is the seventh most common cause of cancer-related deaths worldwide. The incidence and mortality of pancreatic cancer continue to increase, and its 5-yr survival rate remains the lowest among all cancers. N6-methyladenine (m6A) is the most abundant reversible RNA modification in various eukaryotic messenger and long noncoding RNAs and plays crucial roles in the occurrence and development of cancers. However, the role of m6A in pancreatic cancer remains unclear. The present study aimed to explore the role of m6A and its regulators in pancreatic cancer and assess its underlying mol. mechanism associated with pancreatic cancer cell proliferation, invasion, and metastasis. Reduced expression of the m6A demethylase, fat mass and obesity-associated protein (FTO), was responsible for the high levels of m6A RNA modification in pancreatic cancer. Moreover, FTO demethylated the m6A modification of praja ring finger ubiquitin ligase 2 (PJA2), thereby reducing its mRNA decay, suppressing Wnt signaling, and ultimately restraining the proliferation, invasion, and metastasis of pancreatic cancer cells. Altogether, this study describes new, potential mol. therapeutic targets for pancreatic cancer that could pave the way to improve patient outcome. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Synthetic Route of 443-72-1

The Article related to m6a demethylase fto pancreatic cancer pja2 tumorigenesis wnt signaling, n6-methyladenine, pja2, wnt signaling, m6a demethylase fto, pancreatic cancer, Placeholder for records without volume info and other aspects.Synthetic Route of 443-72-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 4, 2020, Liu, Kewei; Cao, Lei; Du, Pufeng; Chen, Wei published an article.Safety of N-Methyl-7H-purin-6-amine The title of the article was im6A-TS-CNN: Identifying the N6-Methyladenine Site in Multiple Tissues by Using the Convolutional Neural Network. And the article contained the following:

N6-methyladenosine (m6A) is the most abundant post-transcriptional modification and involves a series of important biol. processes. Therefore, accurate detection of the m6A site is very important for revealing its biol. functions and impacts on diseases. Although both exptl. and computational methods have been proposed for identifying m6A sites, few of them are able to detect m6A sites in different tissues. With the consideration of the spatial specificity of m6A modification, it is necessary to develop methods able to detect the m6A site in different tissues. In this work, by using the convolutional neural network (CNN), we proposed a new method, called i.m.6A-TS-CNN, that can identify m6A sites in brain, liver, kidney, heart, and testis of Homo sapiens, Mus musculus, and Rattus norvegicus. In i.m.6A-TS-CNN, the samples were encoded by using the one-hot encoding scheme. The results from both a 5-fold cross-validation test and independent dataset test demonstrate that i.m.6A-TS-CNN is better than the existing method for the same purpose. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Safety of N-Methyl-7H-purin-6-amine

The Article related to homo mus rattus convolutional neural network modeling, convolution neural network, m6a, one-hot encoding, spatial specificity of gene expression, Placeholder for records without volume info and other aspects.Safety of N-Methyl-7H-purin-6-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On August 16, 2020, Guo, Dandan; Yang, Chenxi; Qiu, Ruchen; Huang, Shaohua published an article.Application of 5036-48-6 The title of the article was A novel imidazolium bonding stationary phase derived from N-(3-aminopropyl)-imidazole for hydrophilic interaction liquid chromatography. And the article contained the following:

A novel imidazolium bonding method is proposed for the synthesis of hydrophilic interaction liquid chromatog. (HILIC) stationary phases. One obtained stationary phase (SilprAprImCl) was derived from direct reaction between N-(3-aminopropyl)-imidazole and 3-chloropropylated silica gel. Other two materials (SilprAprImBF4 and SilprAprImTf2N) were obtained from SilprAprImCl by ion exchange reaction, resp. FTIR spectroscopy and elemental anal. afforded the proofs of successful imidazolium immobilization and satisfied bonding efficiency. Various polar compounds such as saccharides, nucleosides, and nucleobases were used to evaluate the retention behaviors of these materials in HILIC mode. Different effects from mobile composition, column temperature, imidazolium unite and paired anions (Cl-, BF4-, and Tf2N-) in imidazolium were proved and discussed. Separation mechanism and the role of the imidazolium ions were also studied in mobile phases with different pH. Moreover, chromatog. stability was evaluated by consecutive injections. Finally, the reliability of these stationary phases was demonstrated by the separation of oligosaccharides in real fructooligosaccharides samples. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Application of 5036-48-6

The Article related to imidazolium stationary phase aminopropylimidazole hilic, hilic, imidazolium group, polar compounds, retention mechanism, stationary phase, Placeholder for records without volume info and other aspects.Application of 5036-48-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On December 31, 2021, Bataglia, L.; Simoes, Z. L. P.; Nunes, F. M. F. published an article.Electric Literature of 443-72-1 The title of the article was Active genic machinery for epigenetic RNA modifications in bees. And the article contained the following:

Epitranscriptomics is an emerging field of investigation dedicated to the study of post-transcriptional RNA modifications. RNA methylations regulate RNA metabolism and processing, including changes in response to environmental cues. Although RNA modifications are conserved from bacteria to eukaryotes, there is little evidence of an epitranscriptomic pathway in insects. Here we identified genes related to RNA m6A (N6-methyladenine) and m5C (5-methylcytosine) methylation machinery in seven bee genomes (Apis mellifera, Melipona quadrifasciata, Frieseomelitta varia, Eufriesea mexicana, Bombus terrestris, Megachile rotundata and Dufourea novaeangliae). In A. mellifera, we validated the expression of methyltransferase genes and found that the global levels of m6A and m5C measured in the fat body and brain of adult workers differ significantly. Also, m6A levels were differed significantly mainly between the fourth larval instar of queens and workers. Moreover, we found a conserved m5C site in the honeybee 28S rRNA. Taken together, we confirm the existence of epitranscriptomic machinery acting in bees and open avenues for future investigations on RNA epigenetics in a wide spectrum of hymenopteran species. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Electric Literature of 443-72-1

The Article related to apis melipona epigenetic rna modification methyltransferase 28s rrna, apis mellifera, rna methylation, bee, epitranscripitomics, m5c, m6a, Placeholder for records without volume info and other aspects.Electric Literature of 443-72-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem