Open AccessDevelopment of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones
Author(s) -
Yulin Ren,
A. Douglas Kinghorn
Publication year - 2020
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/acs.jmedchem.0c01449
Subject(s) - parthenolide , chemistry , terpenoid , triptolide , andrographolide , stereochemistry , cytotoxicity , natural product , pharmacology , biochemistry , in vitro , apoptosis , biology
Naturally occurring terpenoid lactones and their synthetic derivatives have attracted increasing interest for their promising antitumor activity and potential utilization in the discovery and design of new antitumor agents. In the present perspective article, selected plant-derived five-membered γ-lactones and six-membered δ-lactones that occur with terpenoid scaffolds are reviewed, with their structures, cancer cell line cytotoxicity and in vivo antitumor activity, structure-activity relationships, mechanism of action, and the potential for developing cancer chemotherapeutic agents discussed in each case. The compounds presented include artemisinin (ART, 1 ), parthenolide (PTL, 2 ), thapsigargin (TPG, 3 ), andrographolide (AGL, 4 ), ginkgolide B (GKL B, 5 ), jolkinolide B (JKL B, 6 ), nagilactone E (NGL E, 7 ), triptolide (TPL, 8 ), bruceantin (BRC, 9 ), dichapetalin A (DCT A, 10 ), and limonin (LMN, 11 ), and their naturally occurring analogues and synthetic derivatives. It is hoped that this contribution will be supportive of the future development of additional efficacious anticancer agents derived from natural products.