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Synthesis, antimitotic and antivascular activity of 1-(3′,4′,5′-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles

Romagnoli, Romeo, Baraldi, Pier Giovanni, Salvador, Maria Kimatrai, Prencipe, Filippo, Bertolasi, Valerio, Cancellieri, Michela, Brancale, Andrea ORCID:, Hamel, Ernest, Castagliuolo, Ignazio, Consolaro, Francesca, Porcù, Elena, Basso, Giuseppe and Viola, Giampietro 2014. Synthesis, antimitotic and antivascular activity of 1-(3′,4′,5′-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles. Journal of Medicinal Chemistry 57 (15) , pp. 6795-6808. 10.1021/jm5008193

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A new class of compounds that incorporated the structural motif of the 1-(3′,4′,5′-trimethoxtbenzoyl)-3-arylamino-5-amino-1,2,4-triazole molecular skeleton was synthesized and evaluated for their antiproliferative activity in vitro, interactions with tubulin, and cell cycle effects. The most active agent, 3c, was evaluated for antitumor activity in vivo. Structure–activity relationships were elucidated with various substituents on the phenyl ring of the anilino moiety at the C-3 position of the 1,2,4-triazole ring. The best results for inhibition of cancer cell growth were obtained with the p-Me, m,p-diMe, and p-Et phenyl derivatives 3c, 3e, and 3f, respectively, and overall, these compounds were more or less as active as CA-4. Their vascular disrupting activity was evaluated in HUVEC cells, with compound 3c showing activity comparable with that of CA-4. Compound 3c almost eliminated the growth of syngeneic hepatocellular carcinoma in Balb/c mice, suggesting that 3c could be a new antimitotic agent with clinical potential.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: ACS Publications
ISSN: 0022-2623
Date of First Compliant Deposit: 30 March 2016
Last Modified: 11 Nov 2023 03:20

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