88075-95-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure
Fu, Zhangyu,Hou, Yingwei,Ji, Cunpeng,Ma, Mingxu,Tian, Zhenhua,Deng, Mengyan,Zhong, Lili,Chu, Yanyan,Li, Wenbao
, p. 2061 - 2072 (2018/03/26)
Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC50 at 1.56 and 1.72 nM, respectively. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization. Furthermore, the interaction between tubulin and these compounds were elucidated by molecular docking. The binding modes of Compounds 13d and 13e were similar to the co-crystal structure of Compound 1. H-π interaction was observed between the aromatic hydrogen of thiophene moiety with Phe20, which could enhance their binding affinities.
Heterocyclically substituted benzimidazoles, the production and application thereof
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Page column 20, (2010/02/05)
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
Preparation of alkyl-substituted indoles in the benzene portion. Part 5. Efficient preparative procedure for 4-substituted indole derivatives
Fuji,Muratake,Natsume
, p. 2338 - 2343 (2007/10/02)
An effective and short synthetic method for 4-substituted indole derivatives was developed based on the two sequential reactions, i.e. nucleophilic addition of carbanions to common precursor molecules, 3-(1,3-dioxolan-2-yl)-1-[1(phenylsulfonyl)- and 1-[(4
