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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|Titolo:||Synthesis and anti-tumor activities of a series of novel quinoxalinhydrazides|
GAROFALO, Antonio (Corresponding)
|Data di pubblicazione:||2007|
|Citazione:||Synthesis and anti-tumor activities of a series of novel quinoxalinhydrazides / Grande, Fedora; Aiello, Francesca; DE GRAZIA, O; Brizzi, A; Garofalo, Antonio; Neamati, N.. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 15:1(2007), pp. 288-294.|
|Appare nelle tipologie:||1.1 Articolo in rivista|