Recently, we discovered a novel class of anticancer compounds with remarkable potency in a panel of cancer cell lines. A prototype compound, SC144, showed significant in vivo efficacy in mice xenograft models of human breast cancer cells. Herein, we report on a new synthetic route to SC144 and the synthesis of several of its analogues in order to understand required features for activity. 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 dramatic effect on potency.
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|Titolo:||Synthesis and antitumor activities of a series of novel quinoxalinhydrazides|
|Rivista:||BIOORGANIC & MEDICINAL CHEMISTRY|
|Citazione:||F., G., F., A., O., D.G., Brizzi, A., A., G., & N., N. (2006). Synthesis and antitumor activities of a series of novel quinoxalinhydrazides. BIOORGANIC & MEDICINAL CHEMISTRY, 15, 288-294.|
|Appare nelle tipologie:||1.1 Articolo in rivista|