Synthesis and antitumor activity of a series of sulfone analogs of 1,4-naphthoquinone

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Abstract
A series of novel substituted thiochromones and thiochroman-4-ones was synthesized. Compounds were designed as analogs of naphthoquinone and as potential bioreductive alkylating agents and were tested for antitumor activity. The lead compound, 3-(chloromethyl)thiochromone 1,1-dioxide, inhibited Ehrlich ascites tumor [carcinoma] growth by 100% in CF1 male mice at 10(mg/kg)/day i.p. Similarly, 18 of the 29 related compounds demonstrated good activity in this tumor screen. Few definitive structure-activity correlations were evident regarding the nature of the 3-substituent. The 2,3 double bond and a sulfone or sulfoxide were required for activity. Four of the compounds synthesized showed marginal but significant activity against P-388 lymphocytic leukemia [mouse].

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