Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives

作者：dos Santos Silva Thiago David; Bomfim Larissa Mendes; Borges da Cruz Rodrigues Ana Carolina; Dias Rosane Borges; Schlaepfer Sales Caroline Brandi; Gurgel Rocha Clarissa Aralujo; Pereira Soares Milena Botelho; Bezerra Daniel Pereira; de Oliveira Cardoso Marcos Verissimo; Lima Leite Ana Cristina; Gadelha Militao Gardenia Carmen

来源：Toxicology and Applied Pharmacology, 2017, 329: 212-223.

DOI：10.1016/j.taap.2017.06.003

• 2-Pyridyl 2,3-thiazoles
• HepG2
• Antitumor
• Cytotoxicity
• Liver Cancer
• Toxicity

A total of 24 hybrid compounds containing pyridyl and 1,3-thiazole moieties were screened against HL-60 (leukemia), MCF-7 (breast adenocarcinoma), HepG2 (hepatocellular carcinoma), NCI-H292 (lung carcinoma) human tumor cell lines and non-tumor cells (PBMC, human peripheral blood mononuclear cells). Most of them were highly potent in at least one cell line tested (IC50 <= 3 mu M), being HL-60 the most sensitive and HepG2 the most resistant cell line. Among them, TAP-07 and TP-07 presented cytotoxic activity in all tumor cell lines, including HepG2 (IC50 2.2 and 5.6 mu M, respectively) without antiproliferative effects to normal cells (PBMC) (IC50 > 30 mu M), making TAP-07 and TP-07, the compounds with the most favorable selectivity index. TAP-07 and TP-07 induced apoptosis in HepG2 cells and presented in vivo antitumor activity in hepatocellular xenograft cancer model in C.B-17 severe combined immunodeficient mice. Systemic toxicological verified by biochemical and histopathological techniques reveled no major signs of toxicity after treatment with TAP-07 and TP-07. Together the results indicated the anti-liver cancer activity of 2-pyridyl 2,3-thiazole derivatives.

• 出版日期2017-8-15