Synthesis and biological evaluation of novel withangulatin A derivatives as potential anticancer agents.
Bioorg Chem
; 108: 104690, 2021 03.
Article
em En
| MEDLINE
| ID: mdl-33592485
ABSTRACT
Novel withangulatin A (WA) derivatives were synthesized and evaluated for antiproliferative activity against four human cancer cell lines (U2OS, MDA-MB-231, HepG2, and A549). Among these derivatives, 10 exhibited the most potent antiproliferative activity, with an IC50 value of 74.0 nM against the human breast cancer cell line MDA-MB-231 and potency that was 70-fold that of WA (IC50 = 5.22 µM). Moreover, 10 caused G2-phase cell cycle arrest in a concentration-dependent manner and induced the apoptosis of MDA-MB-231 cells by increasing intracellular reactive oxygen species (ROS). Compound 10 showed a high selectivity index (SI = 267.03) for breast cancer MDA-MB-231 cells. These results suggest that 10 is a promising anticancer agent.
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MEDLINE
Assunto principal:
Pregnenos
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Antineoplásicos
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article