Natural-product-inspired potent anticancer congeners: chronological advancements, structure-activity relationship (SAR) studies and future perspectives.

Cancer is among the leading causes of mortality and morbidity globally. Natural products have played a significant role in bringing novel therapies to the clinic for the treatment of various types of cancer. However, several natural products have low potency, chemical instability, poor pharmacokinetics, and high toxicity. Therefore, a natural-product-inspired strategy has been utilized to overcome the limitations of natural products in cancer drug discovery. Herein, we present a critical review to describe how medicinal chemists designed anti-cancer agents via a natural-product-inspired strategy. We have also illustrated how this approach is used to overcome drug resistance in cancer. The natural product-inspired analogues/derivatives were classified into different categories. Our focus extends to reviewing the design strategies, in vitro/in vivo results, and structure-activity relationship (SAR) studies of natural-product-inspired molecules as anti-cancer agents. We expect that this review will inspire the development of more effective and diversified anti-cancer agents.