Hu, Cui published the artcileDesign, synthesis and anti-cancer evaluation of novel podophyllotoxin derivatives as potent tubulin-targeting agents, SDS of cas: 1798-04-5, the publication is Medicinal Chemistry Research (2018), 27(2), 351-365, database is CAplus.
A series of podophyllotoxin derivatives (M1-M16) that were selectively acylated by various phenoxy acids at the C-4 position of podophyllotoxin were synthesized, and their biol. activities were also evaluated. Among them, compound M4 showed the most potent anti-cancer activity against HeLa cells with an IC50 value of 1.64 ¡À 0.41 ¦ÌM. Addnl., flow cytometry anal. results indicated that it could cause a remarkable cell cycle arrest at G2/M phase, but the effect on apoptosis inducing was not significant. Moreover, the expression of cell cycle relative protein CDK1 was up regulated while cyclin B1 and Cdc25C, two proteins required for mitotic initiation were down regulated. Furthermore, the confocal assay and extracellular polymerized tubulin expression anal. also demonstrated that M4 was a potent tubulin polymerization inhibitor and the effect was comparable to that of colchicine. Finally, docking simulation results showed that M4 could nicely bind to the colchicine binding site of tubulin which further confirmed the tubulin inhibition activity of M4. Podophyllotoxin-phenoxyacid analogs.
Medicinal Chemistry Research published new progress about 1798-04-5. 1798-04-5 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 2-(4-(tert-Butyl)phenoxy)acetic acid, and the molecular formula is C12H16O3, SDS of cas: 1798-04-5.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia