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

MH Holshouser, LJ Loeffler, IH Hall

文献索引：Holshouser, Mark H.; Loeffler, Larry J.; Hall, Iris H. Journal of Medicinal Chemistry, 1981 , vol. 24, # 7 p. 853 - 858

全文：HTML全文

被引用次数: 40

摘要

A series of novel substituted thiochromones and thiochroman-4-ones was synthesized. Compounds were designed as analogues of naphthoquinone and as potential “bioreductive alkylating agents” and were tested for antitumor activity. The lead compound, 3- (chloromethyl) thiochromone 1, l-dioxide (4), inhibited Ehrlich ascites tumor growth by 100% in CF1 male mice at 10 (mg/kg)/day ip. Similarly, 18 of the 29 related compounds ...