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

Jiali Ji; Farrukh Sajjad; Qun You; Dong Xing; Hui Fan; Alavala G.K. Reddy; Wenhao Hu; Suzhen Dong

doi:10.1002/ardp.202000136

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

Jiali Ji, Farrukh Sajjad, Qun You, Dong Xing, Hui Fan, Alavala G.K. Reddy, Wenhao Hu, Suzhen Dong

School of Chemistry and Molecular Engineering

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Abstract

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 IC₅₀ 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.

Original language	English
Article number	2000136
Journal	Archiv der Pharmazie
Volume	353
Issue number	12
DOIs	https://doi.org/10.1002/ardp.202000136
State	Published - Dec 2020

Keywords

apoptosis
cell cycle arrest
cytotoxicity
pyrroles
pyrrolidines

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/ardp.202000136

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title = "Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents",

abstract = "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 IC50 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.",

keywords = "apoptosis, cell cycle arrest, cytotoxicity, pyrroles, pyrrolidines",

author = "Jiali Ji and Farrukh Sajjad and Qun You and Dong Xing and Hui Fan and Reddy, \{Alavala G.K.\} and Wenhao Hu and Suzhen Dong",

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doi = "10.1002/ardp.202000136",

language = "英语",

volume = "353",

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T1 - Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents

AU - Ji, Jiali

AU - Sajjad, Farrukh

AU - You, Qun

AU - Xing, Dong

AU - Fan, Hui

AU - Reddy, Alavala G.K.

AU - Hu, Wenhao

AU - Dong, Suzhen

PY - 2020/12

Y1 - 2020/12

N2 - 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 IC50 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.

AB - 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 IC50 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.

KW - apoptosis

KW - cell cycle arrest

KW - cytotoxicity

KW - pyrroles

KW - pyrrolidines

UR - https://www.scopus.com/pages/publications/85089157813

U2 - 10.1002/ardp.202000136

DO - 10.1002/ardp.202000136

M3 - 文章

C2 - 32776576

AN - SCOPUS:85089157813

SN - 0365-6233

VL - 353

JO - Archiv der Pharmazie

JF - Archiv der Pharmazie

IS - 12

M1 - 2000136

ER -

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

Abstract

Keywords

UN SDGs

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