Synthesis and anti-tumor activities of a series of novel quinoxalinhydrazides

Recently, we discovered a novel class of anticancer compounds with remarkable potency in a panel of cancer cell lines. Aprototype compound, SC144, showed significant in vivo efficacy in mice xenograft models of human breast cancer cells. Herein, wereport on a new synthetic route to SC144 and the synthesis of several of its analogues in order to understand required features foractivity. A one-step coupling of 7-fluoro-4-chloropyrrolo[1,2-a]quinoxaline with pyrazin-2-carbohydrazide improved the yield significantly.Although several of the analogues showed significant activities, modification of the heteroacyl moiety had a dramaticeffect on potency.