A Supramolecular Nanomedicine Based on Bendamustine and MDM2-Targeted D-peptide Inhibitor for Breast Cancer Therapy was written by Zhou, Yunjiang;Chen, Yaxin;Huang, Xing;Tan, Yingying;Hu, Rong;Li, Chong;Niu, Miao-Miao. And the article was included in Advanced Healthcare Materials in 2021.Electric Literature of C16H21Cl2N3O2 The following contents are mentioned in the article:
Bendamustine (BEN) is a FDA-approved bifunctional DNA-alkylating chemotherapy drug, but it suffers from short half-life, instability, and poor biocompatibility in the clin. application. Due to unique biostability of D-amino acid-containing peptides (D-peptides), constructing D-peptide-small mol. drug conjugates is emerging as a promising strategy for cancer therapy. Here, a high-affinity MDM2-targeted D-peptide (peptide 5) is discovered by applying structure-based drug design (SBDD). Taking the advantages of D-amino acids, a novel self-assembling D-peptide-small mol. drug conjugate (BEN-FF-peptide 5) is developed by simultaneously conjugating small mol. drug BEN and peptide 5 to the self-assembling peptide. In vitro results demonstrate that BEN-FF-peptide 5 exhibits superior cellular uptake ability, good biostability in human serum and strong inhibitory effect on the growth of human breast cancer (MCF-7) cells. In vivo study reveals that BEN-FF-peptide 5 significantly inhibits the growth of MCF-7 cells-derived xenograft in nude mice with no obvious side effects. This work provides a useful strategy to construct D-peptide-small mol. drug conjugates for high-efficacy and low-toxicity cancer therapy. 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: 16506-27-7Electric Literature of 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 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 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).Electric Literature of C16H21Cl2N3O2
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem