Resumo:
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.
