Synthesis, in vitro antiproliferative and antimycobacterial activity of thiazolidine-2,4dione and hydantoin derivatives

New 2H-chromene derivatives bearing thiazolidine-2,4-dione or hydantoin moieties were synthesized and the structures were confirmed by H-1 NMR and C-13 NMR as well as 2D NMR, FTIR. and HR-ESI-MS spectra. The compounds were evaluated for their in vitro cytotoxicity against four human cancer cell lines, namely HL-60 (acute promyelocyte leukemia), REH (lymphoid leukemia), K-562 (chronic myeloid leukemia) and EJ (urinary bladder carcinoma). The 2H-chromene derivative containing thiazolidine-2,4-dione ring 5 was potent against a panel of three cancer cell lines, with an IC50 in the range of 13.1-39.6 mu M and exhibited pronounced antiproliferative activity against lymphoid leukemia (REH cell line) with an 1050 value of 13.1 mu M. The hydantoin containing 2H-chromene derivative 7 having an IC50 value of 83.7 mu M was highly effective against chronic myeloid leukemia K-562. Compounds 5 and 7 also demonstrated significant antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain with minimum inhibitory concentration (MIC) ranging from 0.29 and 0.36 mu M, respectively.