Author(s):
Silva, Thiago David dos Santos ; Bomfim, Larissa Mendes ; Rodrigues, Ana Carolina Borges da Cruz ; Dias, Rosane Borges ; Sales, Caroline Brandi Schlaepfer ; Rocha, Clarissa Araújo Gurgel ; Soares, Milena Botelho Pereira ; Bezerra, Daniel Pereira ; Cardoso, Marcos Veríssimo de Oliveira ; Leite, Ana Cristina Lima ; Militão, Gardenia Carmen Gadelha ; Silva, Thiago David dos Santos ; Bomfim, Larissa Mendes ; Rodrigues, Ana Carolina Borges da Cruz ; Dias, Rosane Borges ; Sales, Caroline Brandi Schlaepfer ; Rocha, Clarissa Araújo Gurgel ; Soares, Milena Botelho Pereira ; Bezerra, Daniel Pereira ; Cardoso, Marcos Veríssimo de Oliveira ; Leite, Ana Cristina Lima ; Militão, Gardenia Carmen Gadelha
Date: 2018
Origin: Oasisbr
Subject(s): 2-Pyridyl 2,3-thiazoles; HepG2; Cytotoxicity; Antitumor; Liver Cancer; Toxicity
Description
Submitted by Renorbio (renorbioba@ufba.br) on 2018-05-02T18:48:24Z No. of bitstreams: 1 ANTI-LIVER CANCER ACTIVITY IN VITRO AND IN VIVO INDUCED BY 2-PYRIDYL 2,3-THIAZOLE DERIVATIVES.pdf: 2793458 bytes, checksum: fcbb9a4336522af9d68dd7cdd4ded487 (MD5)
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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 μM), 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 μM, respectively) without antiproliferative effects to normal cells (PBMC) (IC50 N 30 μM),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 immunodeficientmice. Systemic toxicological verified by biochemical and histopathological techniques reveled nomajor signs of toxicity after treatmentwith TAP-07 and TP-07. Together the results indicated the anti-liver cancer activity of 2-pyridyl 2,3-thiazole derivatives.
