Pentacyclic Triterpenoids with Nitrogen-Containing Heterocyclic Moiety, Privileged Hybrids in Anticancer Drug Discovery

Abstract

Pentacyclic triterpenoids are well-known phytochemicals with various biological activities commonly found in plants as secondary metabolites. The wide range of biological activities exhibited by triterpenoids has made them the most valuable sources of pharmacological agents. A number of novel triterpenoid derivatives with many skeletal modifications have been developed. The most important modifications are the formation of analogues or derivatives with nitrogen-containing heterocyclic scaffolds. The derivatives with nitrogen-containing heterocyclic compounds are among the most promising candidate for the development of novel therapeutic drugs. About 75% of FDA-approved drugs are nitrogen-containing heterocyclic moieties. The unique properties of heterocyclic compounds have encouraged many researchers to develop new triterpenoid analogous with pharmacological activities. In this review, we discuss recent advances of nitrogen-containing heterocyclic triterpenoids as potential therapeutic agents. This comprehensive review will assist medicinal chemists to understand new strategies that can result in the development of compounds with potential therapeutic efficacy.

Novel A-Ring Chalcone Derivatives of Oleanolic and Ursolic Amides with Anti-Proliferative Effect Mediated through ROS-Triggered Apoptosis

“…The introduction of heterocyclic fragments, especially piperazine, has been demonstrated to enhance anticancer properties [ 31 ]. Recently we have found that modification of triterpenoids to indole derivatives on the A-ring with amidation to C28-amide, as well as the introduction of piperazine or N -methyl-piperazine, have a positive effect on anticancer activity [ 32 , 33 ].…”

Synthesis, Characterization, In Vitro Anticancer Potentiality, and Antimicrobial Activities of Novel Peptide–Glycyrrhetinic-Acid-Based Derivatives

“…Pentacyclic triterpenoids (PTs) are the largest group of natural compounds found in plants. Multiple studies have exhibited that there are a considerable number of PTs revealed significant cytotoxic activity against a variety of cancer cells as well as antitumor efficacy in preclinical animal models [ 5 , 6 , 7 , 8 , 9 ]. They induce their anticancer activity via enhancement of cell apoptosis resulting in suppressing tumor growth.…”

Design, Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives

“…Molecular hybridization is a commonly molecular modification approach to obtain multiple compounds with therapeutic advantages over the two different drugs [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 ]. The novel hybrid molecules have the potential to enhance efficacy, improve safety, be cost-effective and reduce the propensity to elicit resistance relative to the parent drugs [ 9 , 10 ].…”