《Design and Synthesis of New Tubulin Polymerization Inhibitors Inspired from Combretastatin A-4: An Anticancer Agent》 was written by Sharma, Akanksha; Talimarada, Doddabasappa; Yadav, Umesh Prasad; Singh, Nidhi; Reddy, A. Sudharshan; Bag, Debojyoti; Biswas, Krishna; Baidya, Amit; Borale, Asha N.; Shinde, Dhananjay; Singh, Sandeep; Holla, Harish. Formula: C5H6O2This research focused ontriazole substituted aryl dihydroisoxazole preparation tubulin polymerization inhibitor antitumor; human mol docking. The article conveys some information:
A series of 30 small hybrid mols. I [R = (CH2)2CH(Me)2, cyclopropyl, 4-BrC6H4, etc.; R1 = H, Cl, OMe; R2 = R4 = H, OMe, R3 = H, Cl, Me, OMe, NO2] were synthesized inspired from Combretastatin A-4 (CA-4), where ethylene-bridge of CA-4 was replaced with two five-membered heterocyclic rings, viz. isoxazoline and 1,2,3-triazole. These were joined by a methylene linker, with substitutions at trisubstituted Ph ring and monosubstituted Ph ring position of CA-4. The new mol. entities had shown significant cytotoxicity to cancer cell from the IC50 0.49μM-3.17μM with 1-((4,5-dihydro-3-(2,5-dimethoxyphenyl)isoxazol-5-yl)methyl)-4-(4-methoxyphenyl)-1H-1,2,3-triazole displayed IC50 0.422±0.07μM for A-549 -lung cancer cell line and IC50 0.498±0.03μM for MDA-MB-231-breast cancer cell line. The western blot anal., confocal staining and also by in vitro tubulin polymerization assay established the target specificity of the mols. as a tubulin polymerization inhibitor. Mol. docking and mol. dynamics studies confirmed the binding interaction patterns of these mols. at the Colchicine binding site of tubulin and have correlated the observed exptl. result with variation in structure satisfactorily. In addition to this study using Ethyl propiolate, there are many other studies that have used Ethyl propiolate(cas: 623-47-2Formula: C5H6O2) was used in this study.
Ethyl propiolate(cas: 623-47-2) is a clear colorless to pale yellow liquid that is soluble in ethanol, ether and chloroform. It an important organic chemical raw material and pharmaceutical intermediate. Ethyl propargylate is obtained by oxidation of propargyl alcohol to propargylic acid followed by esterification.Formula: C5H6O2
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