Unknown

Dataset Information

0

Design, Synthesis and Biological Evaluation of Novel 4-Substituted Coumarin Derivatives as Antitumor Agents.


ABSTRACT: Herein, fifteen new compounds containing coumarin, 1,2,3-triazole and benzoyl- substituted arylamine moieties were designed, synthesized and tested in vitro for their anticancer activity. The results showed that all tested compounds had moderate antiproliferative activity against MDA-MB-231, a human breast cancer cell line, under both normoxic and hypoxic conditions. Furthermore, the 4-substituted coumarin linked with benzoyl 3,4-dimethoxyaniline through 1,2,3-triazole (compound 5e) displayed the most prominent antiproliferative activities with an IC50 value of 0.03 ?M, about 5000 times stronger than 4-hydroxycoumarin (IC50 > 100 ?M) and 20 times stronger than doxorubicin (IC50 = 0.60 ?M). Meanwhile, almost all compounds revealed general enhancement of proliferation-inhibiting activity under hypoxia, contrasted with normoxia. A docking analysis showed that compound 5e had potential to inhibit carbonic anhydrase IX (CA IX).

SUBMITTER: An R 

PROVIDER: S-EPMC6225359 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature

altmetric image

Publications

Design, Synthesis and Biological Evaluation of Novel 4-Substituted Coumarin Derivatives as Antitumor Agents.

An Ran R   Hou Zhuang Z   Li Jian-Teng JT   Yu Hao-Nan HN   Mou Yan-Hua YH   Guo Chun C  

Molecules (Basel, Switzerland) 20180906 9


Herein, fifteen new compounds containing coumarin, 1,2,3-triazole and benzoyl- substituted arylamine moieties were designed, synthesized and tested in vitro for their anticancer activity. The results showed that all tested compounds had moderate antiproliferative activity against MDA-MB-231, a human breast cancer cell line, under both normoxic and hypoxic conditions. Furthermore, the 4-substituted coumarin linked with benzoyl 3,4-dimethoxyaniline through 1,2,3-triazole (compound <b>5e</b>) displ  ...[more]

Similar Datasets

| S-EPMC9611003 | biostudies-literature
| S-EPMC8291583 | biostudies-literature
| S-EPMC6596340 | biostudies-literature
| S-EPMC6891324 | biostudies-literature
| S-EPMC6680717 | biostudies-literature
| S-EPMC8725855 | biostudies-literature
| S-EPMC9268013 | biostudies-literature
| S-EPMC6482410 | biostudies-literature
| S-EPMC6271447 | biostudies-literature
| S-EPMC10478630 | biostudies-literature