Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship...

The synthesis of various substituted Biginelli 3,4-dihydropyrimidinone/thione and Hantzsch 1,4dihydropyridine derivatives has been achieved using a modified procedure in the presence of potassium ter-butoxide (tBuOK) as a catalyst under solvent-free conditions, in good to excellent yields.

A simple protocol for the efficient preparation of aryl and heteroaryl substituted dihydropyrimidinone has been achieved via initial Knoevenagel, subsequent addition, and final cyclization of aldehyde, ethylcyanoacetate, and guanidine nitrate in the presence of piperidine as a catalyst in solvent-free under microwave irradiation. The synthesized compounds showed a good anti-inflammatory, antiba...

A series of chalcones, dihydropyrimidinone and dihydropyrimidinethione derivatives were synthesized in good yields by Claisen Schmidt reaction of acetophenones with substituted aldehydes in the presence of sodium hydroxide in water-ethanol mixture followed by the condensation reaction of chalcones with urea and thiourea in ethanol respectively. The structures of the synthesized compounds were e...

Carbon quantum dots have been conjugated with medicinal dihydropyrimidinone molecules to formulate a multifunctional anticancer drug. Benign CQDs impart fluorescence properties, which enable the composite be used for bioimaging.

Hsp90 C-terminal ligands are potential new anti-cancer drugs alternative to the more studied N-terminal inhibitors. Here we report the identification of a new dihydropyrimidinone binding the C-terminus, which is not structurally related to other well-known natural and nature-inspired inhibitors of this second druggable Hsp90 site.

The Biginelli reaction, which is a three-component reaction for the synthesis of dihydropyrimidinone and corresponding dihydropyrimidinethiones (DHPMs) is known for more than a century. A large number researchers have shown consistent attention towards the study of Biginelli reaction, leading towards structurally diversified molecular libraries of DHPMs and it’s analogues, having significant bi...

Dihydropyrimidinones and dihydropyrimidinethiones generated from the Biginelli reactions of perfluorooctanesulfonyl-attached benzaldehydes are used as common intermediates for post-condensation modifications such as cycloaddition, Liebeskind-Srogl reaction and Suzuki coupling to form biaryl-substituted dihydropyrimidinone, dihydropyrimidine, and thiazolopyrimidine compounds. The high efficiency...

A new facile cost-effective method for the oxidation of acetyl and carboethoxy derivatives of 3,4dihydropyrimidin-2(1H)-ones (DHPMs) by using potassium peroxydisulfate in water as solvent under microwave irradiation has been developed. Whereas the presence of the acetyl group instead of the carboethoxy group in position 5 decreases the rate of oxidation, the nature of the additional subtituent ...