1. Academic Validation
  2. Synthesis and antitumor activities of a series of novel quinoxalinhydrazides

Synthesis and antitumor activities of a series of novel quinoxalinhydrazides

  • Bioorg Med Chem. 2007 Jan 1;15(1):288-94. doi: 10.1016/j.bmc.2006.09.073.
Fedora Grande 1 Francesca Aiello Osvaldo De Grazia Antonella Brizzi Antonio Garofalo Nouri Neamati
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università della Calabria, 87036 Arcavacata di Rende (Cs), Italy.
Abstract

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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