《Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors》 was written by El-Abd, Azhar O.; Bayomi, Said M.; El-Damasy, Ashraf K.; Mansour, Basem; Abdel-Aziz, Naglaa I.; El-Sherbeny, Magda A.. Application of 109-01-3This research focused ontrimethoxyphenylthiazole preparation antitumor SAR tubulin polymerization inhibition mol docking. The article conveys some information:
A new series of 2,4-disubstituted thiazole derivatives I [R = 2-chloroacetyl, 2-(butylamino)acetyl, 2-piperazin-1-ylacetyl, etc.] containing 4-(3,4,5-trimethoxyphenyl) moiety was synthesized and evaluated for their potential anticancer activity as tubulin polymerization inhibitors. All designed compounds I were screened for cytotoxic activity against four human cancer cell lines, namely, HepG2, MCF-7, HCT116, and HeLa, using 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay, with combretastatin A-4 as a reference drug. Compounds I [R = 2-(isopropylamino)acetyl, 2-[4-(4-fluorophenyl)piperazin-1-yl]acetyl, 2-(4-nitroanilino)acetyl, 2-hydrazinoacetyl, 2-[(2Z)-2-(5-chloro-2-oxo-indolin-3-ylidene)hydrazino]acetyl, 2-[(2Z)-2-(5-methyl-2-oxo-indolin-3-ylidene)hydrazino]acetyl] showed superior activity against the tested cell lines, with IC50 values ranging from 3.35 ± 0.2 to 18.69 ± 0.9 μM. Further investigation for the most active cytotoxic agents as tubulin polymerization inhibitors was also performed in order to explore the mechanism of their antiproliferative activity. The obtained results suggested that compounds I [R = 2-(isopropylamino)acetyl, 2-(4-nitroanilino)acetyl, 2-[(2Z)-2-(5-chloro-2-oxo-indolin-3-ylidene)hydrazino]acetyl] remarkably inhibit tubulin polymerization, with IC50 values of 2.95 ± 0.18, 2.00 ± 0.12, and 2.38 ± 0.14 μM, resp., which exceeded that of the reference drug combretastatin A-4 (IC50 2.96 ± 0.18 μM). Mol. docking studies were also conducted to investigate the possible binding interactions between the targeted compounds and the tubulin active site. The interpretation of the results showed clearly that compounds I [R = 2-(4-nitroanilino)acetyl, 2-[(2Z)-2-(5-chloro-2-oxo-indolin-3-ylidene)hydrazino]acetyl] were identified as the most potent tubulin polymerization inhibitors with promising cytotoxic activity and excellent binding mode in the docking study. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Application of 109-01-3)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Application of 109-01-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics