A century-old one-pot multicomponent Biginelli reaction products still finds a niche in drug discoveries: Synthesis, mechanistic studies and diverse biological activities of dihydropyrimidines
“…Several novel and elegant methods have been developed to improve the yield and reaction conditions of the Biginelli reaction. 9 A wide variety of catalytic systems have been applied for the synthesis of functional DHPMs including homogeneous catalysts and heterogeneous catalysts. 10 However, most of the homogeneous catalysts are corrosive and toxic, non-recoverable, expensive and result in low to moderate yields.…”
New Cu (II) nanodots have been developed by the use of biopolymeric polysaccharide galactomannan. The nanocatalyst Cu(II)NDs@CFG has been developed by one-step clean and sustainable reaction of Cassia fistula galactomannan...
“…Several novel and elegant methods have been developed to improve the yield and reaction conditions of the Biginelli reaction. 9 A wide variety of catalytic systems have been applied for the synthesis of functional DHPMs including homogeneous catalysts and heterogeneous catalysts. 10 However, most of the homogeneous catalysts are corrosive and toxic, non-recoverable, expensive and result in low to moderate yields.…”
New Cu (II) nanodots have been developed by the use of biopolymeric polysaccharide galactomannan. The nanocatalyst Cu(II)NDs@CFG has been developed by one-step clean and sustainable reaction of Cassia fistula galactomannan...
“…12 Multicomponent reactions (MCRs) are key for lead discovery and drug design due to their efficiency, variety, and ability to rapidly generate diverse molecular scaffolds. 13,14 MCRs leads to a product with varied functional groups and structural motifs by reaction with at least three building blocks. 15 This synthetic approach efficiently compiles different chemical libraries, which helps to explore chemical space and identify lead compounds with required pharmacological activity.…”
Our study introduces novel symmetrical and asymmetrical dihydropyridines as breast cancer inhibitors, showing cytotoxicity against MCF-7 cells and EGFR kinase inhibition. Molecular docking and dynamics validate superior binding to Lapatinib.
“…Given this large field of activities, DHPMs are considered a paramount drug target in medicinal chemistry. 6–10 The first work that described the effect of monastrol as an antitumoral compound was reported in 1999. 11 The authors reported the ability of monastrol to interrupt mitosis by inhibiting the motor activity of the kinesin Eg5.…”
Monastrol is a cell-permeable molecule recognized as an inhibitor of mitotic kinesin Eg5, that is over-expressed in tumor cells and is a very promising target for developing new drugs for cancer disease.
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