Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies

• Published in: European journal of medicinal chemistry 2021-10, Vol.221, p.113511-113511, Article 113511
• Main Authors: Arya, Girish Chandra, Kaur, Kamalpreet, Jaitak, Vikas
• Format: Article
• Language: English
• Subjects: Breast cancer; Isoxazole; Mechanism of action; Signalling pathways; Structure-activity relationship; Synthetic strategies
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2021.113511

Breast cancer is the second most leading cause of death among women. Multiple drugs have been approved by FDA for the treatment of BC. The major drawbacks of existing drugs are the development of resistance, toxicity, selectivity problem. The other therapies like hormonal therapy, surgery, radiotherapy, and immune therapy are in use but showed many side effects like bioavailability issues, non-selectivity, pharmacokinetic-pharmacodynamic problems. Therefore, there is an urgent need to develop new moieties that are nonviolent and more effective in the treatment of cancer. Isoxazole derivatives have gain popularity in recent years due to anticancer potential with the least side effects. These derivatives act as an anticancer agent with different mechanisms like inducing apoptosis, aromatase inhibition, disturbing tubulin congregation, topoisomerase inhibition, HDAC inhibition, and ERα inhibition. In this article, we have explored the synthetic strategies, anticancer mechanism of action along with SAR studies of isoxazole derivatives. [Display omitted] •Isoxazole based heterocyclic compounds as anticancer agent.•Synthetic approaches for the synthesis of substituted isoxazole derivatives.•Targets for the anticancer activities of each isoxazole derivative.•SAR and in-vitro studies of isoxazole derivatives based on their mechanism of action have been discussed.•The complete SAR of isoxazole for its anticancer activities is also discussed.