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Updated: Jul 18, 2026

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Structural simplification of bioactive natural products with multicomponent synthesis: dihydropyridopyrazole
Igor V Magedov1, Madhuri Manpadi, Elena Rozhkova
1Department of Organic Chemistry, Timiryazev Agriculture Academy, Moscow 127550, Russia. intelbioscan@mtu-net.ru
Abstract:
A three-component condensation of 5-amino-3-methylpyrazole, tetronic acid, and various aromatic, heteroaromatic, and aliphatic aldehydes leads to the formation of dihydropyridopyrazole analogues of a cytotoxic lignan podophyllotoxin. This new heterocyclic scaffold-based library allows a drastic reduction of the structural complexity of the natural product with the retention of its potent cytotoxic properties. Similarly to podophyllotoxin, the presented analogues induce apoptosis in Jurkat cells.

