Natural product inspired leads in the discovery of anticancer agents: an update

Natural products have emerged as major leads for the discovery and development of new anti-cancer drugs. The plant-derived anti-cancer drugs account for approximately 60% and the quest for new anti-cancer agents is in progress. Anti-cancer leads have been isolated from plants, animals, marine organisms, and microorganisms from time immemorial. The process of semisynthetic modifications of the parent lead has led to the generation of new anti-cancer agents with improved therapeutic efficacy and minimal side effects. The various chemo-informatics tools, bioinformatics, high-throughput screening, and combinatorial synthesis are able to deliver the new natural product lead molecules. Plant-derived anticancer agents in either late preclinical development or early clinical trials include taxol, vincristine, vinblastine, topotecan, irinotecan, etoposide, paclitaxel, and docetaxel. Similarly, anti-cancer agents from microbial sources include dactinomycin, bleomycin, mitomycin C, and doxorubicin. In this review, we highlighted the importance of natural products leads in the discovery and development of novel anti-cancer agents. The semisynthetic modifications of the parent lead to the new anti-cancer agent are also presented. Further, the leads in the preclinical settings with the potential to become effective anticancer agents are also reviewed. Communicated by Ramaswamy H. Sarma

Automated summary

Natural products are crucial for discovering and developing new anti-cancer drugs, with plant-derived drugs accounting for about 60% of the total. Anti-cancer leads have been found in plants, animals, marine organisms, and microorganisms throughout history. By modifying the parent leads, new anti-cancer agents with improved efficacy and fewer side effects can be created. Various techniques such as chemo-informatics, bioinformatics, high-throughput screening, and combinatorial synthesis can be utilized to identify new natural product leads.