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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 (IC 50  = 10–30 μM). Further studies on the SAR of compound  2e  may result in good anticancer activity.

One-pot synthesis and in-vitro anticancer evaluation of 5-(2′-indolyl)thiazoles