Synthesis and antitumor activities of a series of novel quinoxalinhydrazides |
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Authors: | Grande Fedora Aiello Francesca Grazia Osvaldo De Brizzi Antonella Garofalo Antonio Neamati Nouri |
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Affiliation: | Dipartimento di Scienze Farmaceutiche, Università della Calabria, 87036 Arcavacata di Rende (Cs), Italy. |
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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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