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Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents
Author(s) -
Ji Jiali,
Sajjad Farrukh,
You Qun,
Xing Dong,
Fan Hui,
Reddy Alavala G. K.,
Hu Wenhao,
Dong Suzhen
Publication year - 2020
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.202000136
Subject(s) - pyrrolidine , chemistry , pyrrole , apoptosis , combinatorial chemistry , cell cycle checkpoint , cell culture , cell cycle , stereochemistry , cell growth , hl60 , biochemistry , organic chemistry , biology , genetics
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. Pyrrolidines 3h and 3k showed good proliferation inhibitory effects toward 10 cancer cell lines with IC 50 values ranging from 2.9 to 16 μM. Furthermore, pyrrolidine 3k induced 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.