Farooq, Saleem published the artcileDihydropyrimidinones: efficient one-pot green synthesis using Montmorillonite-KSF and evaluation of their cytotoxic activity, Application In Synthesis of 86-51-1, the main research area is Montmorillonite KSF support heteropoly acid catalyst preparation surface area; aldehyde acetoacetate urea heterogeneous catalyst Biginelli reaction green chem; dihydropyrimidinone preparation antitumor cytotoxicity SAR docking.
A simple, efficient, cost-effective, recyclable and green approach was developed for the synthesis of new dihydropyrimidinone analogs I [X = O, S; R = Ph, (E)-2-(4-methoxyphenyl)vinyl, 1-chloro-3,4-dihydronaphthalenyl, etc.] via Biginelli reaction. The methodol. involved a multicomponent reaction catalyzed by “”HPA-Montmorillonite-KSF”” as a reusable and heterogeneous catalyst. This method gave an efficient and much improved modification of the original Biginelli reaction, in terms of yield and short reaction times under solvent free conditions. All the derivatives were subjected to cytotoxicity screening against a panel of four different human cancer cell lines viz. colon (Colo-205), prostate (PC-3), leukemia (THP-1) and lung (A549) to check their effect on percentage growth. MTT [3-(4,5-dimethylthiazol-yl)-diphenyl tetrazoliumbromide] cytotoxicity assay was employed to check IC50 values. Of the synthesized analogs, I [X = O, R = (E)-2-(4-methoxyphenyl)vinyl] showed the best activity with IC50 of 7.1 ± 0.8, 13.1 ± 1.4, 13.8 ± 0.9 and 14.7 ± 1.1μM against lung (A549), leukemia (THP-1), prostate (PC-3) and colon (Colo-205) cancer lines, resp. Synthesized compound I [X = O, R = (E)-2-(4-methoxyphenyl)vinyl] were further checked for its effect on cancer cell properties through clonogenic (colony formation) and scratch motility (wound healing) assays and thereby were found that it reduced both the colony formation and migratory properties of the lung cancer cell line (A549). Mol. docking studies were performed with I [X = O, R = (E)-2-(4-methoxyphenyl)vinyl], which showed its binding mode.
RSC Advances published new progress about Antitumor agents. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application In Synthesis of 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem