Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents

被引：13

作者：

Ji, Jiali ^{[1
]}

Sajjad, Farrukh ^{[1
]}

You, Qun ^{[1
]}

Xing, Dong ^{[1
]}

Fan, Hui ^{[1
]}

Reddy, Alavala G. K. ^{[2
]}

Hu, Wenhao ^{[1
,2
]}

Dong, Suzhen ^{[1
,3
]}

机构：

[1] East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China

[2] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Peoples R China

[3] East China Normal Univ, Key Lab Brain Funct Genom, Minist Educ, Shanghai, Peoples R China

来源：

ARCHIV DER PHARMAZIE | 2020年 / 353卷 / 12期

基金：

上海市自然科学基金;

关键词：

apoptosis; cell cycle arrest; cytotoxicity; pyrroles; pyrrolidines; MULTICOMPONENT REACTIONS; DERIVATIVES;

D O I：

10.1002/ardp.202000136

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of polysubstituted pyrrolidines obtained via ruthenium-catalyzed cascade cyclization of diazo pyruvates and anilines as well as their corresponding pyrrole analogs obtained via dehydration were evaluated for their antiproliferation activities. Pyrrolidines3hand3kshowed good proliferation inhibitory effects toward 10 cancer cell lines with IC(50)values ranging from 2.9 to 16 mu M. Furthermore, pyrrolidine3kinduced cell cycle arrest at the G0/G1 phase and time- and dose-dependent cellular apoptosis in both HCT116 and HL60 cells, suggesting that this type of pyrrolidine structure might be a good candidate for future anticancer therapies.

引用

页数：9

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