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Updated: Mar 9, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, molecular modeling and biological evaluation of two new chicoric acid analogs
Giuliana Righi1, Romina Pelagalli2, Valerio Isoni2
1a CNR-IBPM Department of Chemistry , "Sapienza" Universy of Rome , Rome , Italy.
Abstract:
Two conformationally constrained compounds similar to chicoric acid but lacking the catechol and carboxyl groups were prepared. In these analogues, the single bond between the two caffeoyl fragments has been replaced with a chiral oxirane ring and both aromatic residues modified protecting completely or partially the catechol moiety as methyl ether. Preliminary molecular modelling studies carried out on the two analogues showed interactions near the active site of HIV integrase; however, in comparison with raltegravir, the biological evaluation confirmed that CAA-1 and CAA-2 were unable to inhibit infection at lower concentration.
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