Recently I am researching about BIOLOGICAL EVALUATION; DERIVATIVES; ANALOGS, Saw an article supported by the Natural Science Foundation of Guangdong Province, ChinaNational Natural Science Foundation of Guangdong Province [2018B030311067]; Science and Technology Program of Guangzhou City, China [201707010198]. Recommanded Product: 1-(4-Nitrophenyl)ethanone. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Huo, XS; Jian, XE; Ou-Yang, J; Chen, L; Yang, F; Lv, DX; You, WW; Rao, JJ; Zhao, PL. The CAS is 100-19-6. Through research, I have a further understanding and discovery of 1-(4-Nitrophenyl)ethanone
Y By removing 5-methyl and 6-acetyl groups in our previously reported compound 3, we designed a series of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidine derivatives as potential tubulin polymerization inhibitors. Among them, compound 5e displayed low nanomolar antiproliferative efficacy on HeLa cells which was 166-fold higher than the lead analogue 3. Interestingly, 5e displayed significant selectivity in inhibiting cancer cells over HEK-293 (normal human embryonic kidney cells). In addition, 5e dose-dependently arrested HeLa in G2/M phase through the alterations of the expression levels of p-cdc2 and cyclin B1, and caused HeLa cells apoptosis by regulation of expressions of cleaved PARP. Further evidence demonstrated that 5e effectively inhibited tubulin polymerization and was 3-fold more powerful than positive control CA-4. Moreover, molecular docking analysis indicated that 5e overlapped well with CA-4 in the colchicine-binding site. These studies demonstrated that 2,7-diaryl-[1,2,4]triazolo [1,5-a]pyrimidine skeleton might be used as the leading unit to develop novel tubulin polymerization inhibitors as potential anticancer agents. (C) 2021 Elsevier Masson SAS. All rights reserved.
Recommanded Product: 1-(4-Nitrophenyl)ethanone. About 1-(4-Nitrophenyl)ethanone, If you have any questions, you can contact Huo, XS; Jian, XE; Ou-Yang, J; Chen, L; Yang, F; Lv, DX; You, WW; Rao, JJ; Zhao, PL or concate me.
Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem