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【論文發表】Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores

2019年09月10日 17:37  點擊:[]

Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores

By: Huang, Mingqin; Duan, Shengzu; Ma, Xueqiong; Cai, Bicheng; Wu, Dongmei; Li, Yan; Li, Liang; Zhang, Hongbin; Yang, Xiaodong

MEDCHEMCOMM

Volume: 10 Issue: 6 Pages: 1027-1036

DOI: 10.1039/c9md00112c

Published: JUN 1 2019

Document Type:Article

Abstract

The synthesis of a series of novel aza-brazilan derivatives containing imidazolium salt pharmacophores is presented. The biological activity of such imidazolium salts was further evaluated in vitro against a panel of human tumor cell lines. The results suggest that the electron-withdrawing group on the aza-brazilan moiety, substituted 5,6-dimethyl-benzimidazole ring and substitution of the imidazolyl-3-position with a 4-methylbenzyl group were essential for modulating the cytotoxic activity. Compounds 55 and 39, bearing a 4-methylbenzyl substituent at position-3 of 5,6-dimethyl-benzimidazole, were found to be the most potent compounds with IC50 values of 0.52-1.30 mu M and 0.56-1.51 mu M against four human tumor cell lines investigated. Particularly, compound 57 exhibited inhibitory activity against the MCF-7 cell line with an IC50 value of 0.35 mu M and was 56-fold more sensitive than DDP. Moreover, compound 55 inhibited cell proliferation through inducing G0/G1 cell cycle arrest and apoptosis in SMMC-7721 cells.

Keywords

KeyWords Plus:NITRIC-OXIDE SYNTHASE; CYTOTOXIC ACTIVITY; HYBRID COMPOUNDS; DESIGN; BETA; INHIBITION; DISCOVERY; CELLS

Addresses:

[ 1 ] Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resource, Minist Educ & Yunnan Prov, Kunming 650091, Yunnan, Peoples R China

[ 2 ] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Yunnan, Peoples R China

上一條:【論文發表】Tandem reaction of heterocyclic ketene aminals with diazoesters: Synthesis of pyrimidopyrrolidone derivatives 下一條:【論文發表】An Efficient Route to Isochromene Derivatives via Cascade Radical Cyclization and Radical-Radical Coupling

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