One-pot synthesis and in-vitro anticancer evaluation of 5-(2'-indolyl)thiazoles [electronic resource]

• Ngôn ngữ: eng
• Ký hiệu phân loại: 547.7 Macromolecules and related compounds
• Thông tin xuất bản: Washington, D.C. : Oak Ridge, Tenn. : United States. Dept. of Energy. Office of Science ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2016
• Mô tả vật lý: Size: Article No. 23401 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 260900
• Chủ đề: 1. 60 applied life sciences; 2. Science & technology - other topics

Tóm tắt

A series of 5-(2'-indolyl)thiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of thioamides 3 with 3-tosyloxypentane-2,4-dione 4 led to in situ formation of 5-acetylthiazole 5 which upon treatment with arylhydrazines 6 in polyphosphoric acid resulted in the formation of 5-(2'-indolyl)thiazoles 2. Among the synthesized 5-(2'-indolyl)thiazoles, compounds 2d?f, and 2h exhibited encouraging anticancer activity and also selectivity towards particular cell lines (IC50=10?30?M). Further studies on the SAR of compound 2e may result in good anticancer activity.