期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 5, 页码 1608-1619出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.01.033
关键词
1,4-Naphthoquinone; Lapachol; 1,2,3-Triazoles; Click chemistry; Cancer
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq) Project Universal-MCTI/CNPq [14/2012 (480719/2012-8)]
- Chamada MCTI/CNPq [16/2012]
- CAPES
- Fundacao Cearense de Pesquisa e Cultura (FUNCAP-Edital Pronex)
- Fundacao de Apoio a pesquisa do Estado de Alagoas (FAPEAL, PRONEX)
- Fundacao de Apoio a pesquisa do Estado de Pernambuco (FACEPE, PRONEM)
1,2,3-Triazole-, arylamino- and thio-substituted naphthoquinones (24, 8, and 2 representatives, respectively) were synthesized in moderate yields and evaluated against several human cancer cell lines (blood, ovarian, breast, central nervous system, colon, and prostate cancers and melanoma), showing, for some of them, IC50 values below 2 mu M. The cytotoxic potential of the tested naphthoquinones was also assayed on non-tumor cells such as human peripheral blood mononucluear cells (PBMC) and two murine fibroblast lines (L929 and V79 cells). alpha-Lapachone-and nor-alpha-lapachone-based 1,2,3-triazoles and arylamino-substituted naphthoquinones showed potent cytotoxicity against different cancer cell lines. The compounds may represent promising new lead derivatives for anticancer drug development. The electrochemical properties of selected compounds were evaluated in an attempt to correlate them with antitumor activity. (C) 2014 Elsevier Ltd. All rights reserved.
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