J Med Chem 2020 12 8;63(24):15410-15448. Epub 2020 Dec 8.
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
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, ), parthenolide (PTL, ), thapsigargin (TPG, ), andrographolide (AGL, ), ginkgolide B (GKL B, ), jolkinolide B (JKL B, ), nagilactone E (NGL E, ), triptolide (TPL, ), bruceantin (BRC, ), dichapetalin A (DCT A, ), and limonin (LMN, ), and their naturally occurring analogues and synthetic derivatives. Read More