期刊
NATURAL PRODUCT RESEARCH
卷 36, 期 17, 页码 4410-4416出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2021.1984465
关键词
Chalcone; breast cancer; colon cancer; selectivity index; quantitative structure-activity relationship
资金
- [Agencia Nacional de Investigacion y Desarrollo (ANID)] under [Fondecyt] research grants [3180408, 1161490]
- Pontificia Universidad Catolica de Valparaiso [VRIEA-PUCV 37.0/2017]
Cancer, the second leading cause of death worldwide, has led to the development of novel anticancer agents like chalcone derivatives. Research has shown that chalcones 4w and 4t exhibit high potency and selectivity against Caco-2 and MCF-7 cells, making them attractive candidates for further development as pro apoptotic agents.
Cancer is the second death cause worldwide, with breast and colon cancer among the most prevalent types. Traditional treatment strategies have several side effects that inspire the development of novel anticancer agents derived from natural sources, like chalcone derivatives. For this investigation, twenty-three chalcones (4a-w) were synthesized and evaluated as antiproliferative agents against MCF-7 and Caco-2 cells, finding three and two compounds with similar or higher antiproliferative activity than daunorubicin, while only two chalcones showed better selectivity indexes than daunorubicin on MCF-7. From these results, we developed good-performance QSAR models (r > 0.850, q(2)>0.650), finding several structural features that could modify chalcone activity and selectivity. According to these models, chalcones 4w and 4t have high potency and selectivity against Caco-2 and MCF-7, respectively, which make them attractive candidates for hit-to-lead development of ROS-independent pro apoptotic agents.
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