期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 165, 期 -, 页码 18-30出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.01.001
关键词
Oxadiazoles; Anticancer activity; Mannich bases; Lipophilicity
资金
- FAPEMIG [CEX -APQ-00591-15]
- CAPES
- CNPq
- FAPEMIG-Brazil [CEX APQ 01622/13, CEX APQ 01287/14]
- CNPq (EDITAL MCTI/CNPq) [14/2014]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior - Brazil (CAPES) [001]
- [MCT/FINEP/CT-INFRA 01/2013-REF 0633/13]
A series of1,2,4- and 1,3,4-oxadiazole derivatives were synthesized and evaluated for their anticancer activity. Halogenated 1,2,4-oxadiazoles were obtained from benzonitrile and coupled either lipophilic amines or with aminoalcohols. Lipophilic 1,3,4-oxadiazole derivatives were obtained through the Mannich reactions between 5-(aryl)-1,3,4-oxadiazole-2-thiol and alkylated or acylated amines. The in vitro cytotoxic effects were evaluated against 4T1- mammary carcinoma and CT26 - colon cancer cells. The best results were obtained for the 1,3,4-oxadiazole coupled to alkylated piperazine with 10-14 carbon chain moiety, with IC50 values ranging from 1.6 to 3.55 mu M for the 4T1 cell line, and from 1.6 to 3.9 mu M for the CT26.WT cell line, and selectivity index up to 19. The most potent compounds were investigated with AnnexinV and PI staining as indicative of apoptosis induction. (C) 2019 Published by Elsevier Masson SAS.
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