Synthesis and Structure Determination of Substituted Thiazole Derivatives as EGFR/BRAF^V600E Dual Inhibitors Endowed with Antiproliferative Activity.

ABSTRACT: 2,3,4-trisubstituted thiazoles 3a-i, having a methyl group in position four, were synthesized by the reaction of 1,4-disubstituted thiosemicarbazides with chloroacetone in ethyl acetate/Et₃N at room temperature or in ethanol under reflux. The structures of new compounds were determined using NMR spectroscopy, mass spectrometry, and elemental analyses. Moreover, the structure of compound 3a was unambiguously confirmed with X-ray analysis. The cell viability assay of 3a-i at 50 µM was greater than 87%, and none of the tested substances were cytotoxic. Compounds 3a-i demonstrated good antiproliferative activity, with GI₅₀ values ranging from 37 to 86 nM against the four tested human cancer cell lines, compared to the refer

SUBMITTER: Al-Wahaibi LH 

PROVIDER: S-EPMC10384562 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature