An article Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer WOS:000526982300002 published article about IN-VITRO; AGENT; MECHANISM; INSIGHTS in [Ding, Zhongpeng; Li, Feifei; Zhong, Changjiang; Liu, Yuqian; Zhao, Jianchun; Li, Wenbao] Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Peoples R China; [Li, Wenbao] Qingdao Natl Lab Marine Sci & Technol, Innovat Ctr Marine Drug Screening & Evaluat, Qingdao 266071, Peoples R China; [Li, Feng] Weifang Univ Sci & Technol, Shandong Peninsula Engn Res Ctr Comprehens Brine, Weifang 262700, Shandong, Peoples R China; [Wang, Shixiao; Zhao, Jianchun; Li, Wenbao] Marine Biomed Res Inst Qingdao, Qingdao 266071, Peoples R China in 2020.0, Cited 24.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 3-Pyridinecarboxaldehyde
Plinabulin, a synthetic analog of the marine natural product diketopiperazine phenylahistin, displayed depolymerization effects on microtubules and targeted the colchicine site, which has been moved into phase III clinical trials for the treatment of non-small cell lung cancer (NSCLC) and the prevention of chemotherapy-induced neutropenia (CIN). To develop more potent anti-microtubule and cytotoxic derivatives, the co-crystal complexes of plinabulin derivatives were summarized and analyzed. We performed further modifications of the tert-butyl moiety or C-ring of imidazole-type derivatives to build a library of molecules through the introduction of different groups for novel skeletons. Our structure-activity relationship study indicated that compounds 17o (IC50 = 14.0 nM, NCI-H460) and 17p (IC50 = 2.9 nM, NCI-H460) with furan groups exhibited potent cytotoxic activities at the nanomolar level against various human cancer cell lines. In particular, the 5-methyl or methoxymethyl substituent of furan group could replace the alkyl group of imidazole at the 5-position to maintain cytotoxic activity, contradicting previous reports that the tert-butyl moiety at the 5-position of imidazole was essential for the activity of such compounds. Immunofluorescence assay indicated that compounds 17o and 17p could efficiently inhibit microtubule polymerization. Overall, the novel furan-diketopiperazine-type derivatives could be considered as a potential scaffold for the development of anti-cancer drugs.
Welcome to talk about 500-22-1, If you have any questions, you can contact Ding, ZP; Li, FF; Zhong, CJ; Li, F; Liu, YQ; Wang, SX; Zhao, JC; Li, WB or send Email.. Recommanded Product: 3-Pyridinecarboxaldehyde
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem