Synthesis and anticancer activity of a novel class of flavonoids: 2,4-Diarylchromane[4,3-d]-Δ1,9b-1,2,3-thiadiazolines

Abstract: A series of 2,4-diarylchromane[4,3-d]-Δ1,9b-1,2,3-thiadiazolines have been synthesized by cyclization of corresponding 2-arylchroman-4-one-arylhydrazones with SOCl2 then treated with alcohol. All the compounds have been tested for their antiproliferative activity in vitro against six human tumor cell lines, and the highly potent derivative 11a exhibited in vivo inhibitory effect on tumor growth. Mechanism research indicated that it is due to 11a that induces DNA fragmentation. [Copyright &y& Elsevier]