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Synthesis 2019; 51(02): 573-577
DOI: 10.1055/s-0037-1610291
DOI: 10.1055/s-0037-1610291
paper
Synthesis and Antitumor Activity of Novel 1-Substituted 3-(4,5-Substituted 1,2,4-Triazol-3-yl)-β-carboline Derivatives
Authors
This work was supported by Fundação Araucária (Brazil, PR) and Fundação de Amparo à Pesquisa de São Paulo (FAPESP).
Further Information
Publication History
Received: 04 July 2018
Accepted after revision: 30 August 2018
Publication Date:
26 September 2018 (online)
Abstract
Schiff bases, 1,2,4-triazolo[4,3-d][1,2,3,4]thiatriazoles, and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles carrying the β-carboline nucleus were synthesized from 3-(4-amino-5-mercapto-1,2,4-triazol-3-yl)-β-carbolines. The compounds were evaluated for their in vitro antitumor activity against eight human cancer cell lines. The 1,2,4-triazolo[4,3-d][1,2,3,4]thiatriazole derivatives showed a broad spectrum of antitumor activity, with GI50 values lower than 13 μM for all cell lines tested. In general, all tested compounds showed potent activity against the breast (MCF-7) cancer cell line, with GI50 values in the range of 2.07 to 4.58 μM.
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