Synthesis and antitumor activity of some new substituted quinolin-4-one and 1,7-naphthyridin-4-one analogs

The synthesis of some new analogs of quinolin-4-one and 1,7-naphthyridin-4- one is described. The prepared compounds were tested for their in vitro ant itumor and cdc2 kinase or cdc25 phosphatase inhibitory activity. Compound e thyl 7-oxo-2,3-dihydro-7H-pyrido [1,2,3-de] [2,3-b]pyrido-1,4-thiazine-6-ca rboxylate (6b) showed antitumor activity against CNS SNB-75, breast T-47D, and lung NCI-H522 cancer cell lines with GI(50) values of 8.3, 17.6 and 22. 7 mu M, respectively. Meanwhile, the compounds ethyl 4-oxo-8-phenylthio-1H, 4H-quinoline-3-carboxylate (11a) and 4-oxo-8-phenylthio-1H,4H-1,7-naphthyri dine-3-carboxylic acid (12b) have proved to be cdc25 phosphatase inhibitors at IC50 values of 11 and 5 mu M, respectively.