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.

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

GRANDE, Fedora;AIELLO, Francesca;DE GRAZIA O;GAROFALO, Antonio
;
2007-01-01

Abstract

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11770/123301
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