期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 19, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127454
关键词
1,2,3-Triazole; Chalcone; Hybridization; Prostate cancer; Endocrine cancer
资金
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior-Brasil, Brazil (CAPES) [001]
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico, Brazil (CNPq)
- Fundacao de Amparo a Pesquisa do Espirito Santo, Brazil (FAPES)
Prostate cancer is an important cause of death in the male population and for which there is no satisfactory chemotherapy. Herein a new series of chalcone hybrids containing 2H-1,2,3-triazole core as the ring B has been synthesized and evaluated in vitro against PC-3 prostate cancer cell line. Compounds 4a, 4c and 4e significantly reduced cell viability and showed IC50 of 28.55, 15.64 and 25.56 mu M, respectively. The structure-activity relationship supported by computational chemistry points that the polarity of the molecular surface area should have some relevance to the efficiency of the compounds, in particular the ratio of the partial positive charge sites and the total molecular surface area exposed to the cell environment.
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