Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs

Lei Wang; Ying Huang; Jie Zhang; Linjiang Tong; Yi Chen; Wei Lu; Qingqing Huang

doi:10.1016/j.bmcl.2014.01.049

Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs

Lei Wang
, Ying Huang
, Jie Zhang
, Linjiang Tong
, Yi Chen^*
, Wei Lu
, Qingqing Huang

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

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

12 Scopus citations

Abstract

In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.

Original language	English
Pages (from-to)	1597-1599
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2014.01.049
State	Published - 15 Mar 2014

Keywords

Antitumor
C-7-heteroaryl-substituted camptothecin
Camptothecin
Suzuki coupling

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10.1016/j.bmcl.2014.01.049

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title = "Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs",

abstract = "In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.",

keywords = "Antitumor, C-7-heteroaryl-substituted camptothecin, Camptothecin, Suzuki coupling",

author = "Lei Wang and Ying Huang and Jie Zhang and Linjiang Tong and Yi Chen and Wei Lu and Qingqing Huang",

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T1 - Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs

AU - Wang, Lei

AU - Huang, Ying

AU - Zhang, Jie

AU - Tong, Linjiang

AU - Chen, Yi

AU - Lu, Wei

AU - Huang, Qingqing

PY - 2014/3/15

Y1 - 2014/3/15

N2 - In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.

AB - In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition.

KW - Antitumor

KW - C-7-heteroaryl-substituted camptothecin

KW - Camptothecin

KW - Suzuki coupling

UR - https://www.scopus.com/pages/publications/84895820856

U2 - 10.1016/j.bmcl.2014.01.049

DO - 10.1016/j.bmcl.2014.01.049

M3 - 文章

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AN - SCOPUS:84895820856

SN - 0960-894X

VL - 24

SP - 1597

EP - 1599

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 6

ER -

Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs

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Keywords

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