Design, Synthesis and Biological Activity of (20S,21S)-7-Cyclohexyl-21-fluorocamptothecin Carbamates as Potential Antitumor Agents | Health & Environmental Research Online (HERO)

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Citation
Tags

HERO ID

7292724

Reference Type

Journal Article

Title

Design, Synthesis and Biological Activity of (20S,21S)-7-Cyclohexyl-21-fluorocamptothecin Carbamates as Potential Antitumor Agents

Author(s)

Ma, H; Chen, B; Wang, Y; Wang, C; Yao, J; Zhang, W; Miao, Z

Year

2020

Is Peer Reviewed?

Yes

Journal

Chemistry & Biodiversity
ISSN: 1612-1872
EISSN: 1612-1880

Publisher

Wiley-VCH Verlag

Volume

Issue

Page Numbers

e2000068

Language

English

PMID

32342605

DOI

10.1002/cbdv.202000068

Web of Science Id

WOS:000538744600001

Abstract

(20S,21S)-7-Cyclohexyl-21-fluorocamptothecin was discovered by a fluorine drug design strategy with potent antitumor activity and increased metabolic stability. In continuous efforts to find novel antitumor agents derived from natural product camptothecin, 20-carbamates of the active compound (20S,21S)-7-cyclohexyl-21-fluorocamptothecin have been designed and synthesized. Among them, one compound with the diethylamino group showed greater antiproliferative activity than the other 20-carbamate derivatives. The following biological activity assays indicated that the above compound is a valuable lead compound with excellent Topo I inhibitory activity and solution stability.

Keywords

biological activity; camptothecin; carbamate; drug design; fluorine-containing drug; 7 cyclohexyl 21 fluorocamptothecin; antineoplastic agent; camptothecin; carbamic acid derivative; unclassified drug; antineoplastic activity; antiproliferative activity; Article; controlled study; drug design; drug synthesis; human; human cell; IC50