Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghhudha, Bathinda, Pb, 151401, India.
Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghhudha, Bathinda, Pb, 151401, India.
Eur J Med Chem. 2021 Oct 5;221:113511. doi: 10.1016/j.ejmech.2021.113511. Epub 2021 May 6.
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.
乳腺癌是女性死亡的第二大主要原因。美国食品药品监督管理局已批准多种药物用于治疗乳腺癌。现有药物的主要缺点是耐药性、毒性和选择性问题。其他疗法，如激素疗法、手术、放射疗法和免疫疗法也在使用，但显示出许多副作用，如生物利用度问题、非选择性、药代动力学-药效学问题。因此，迫切需要开发新的药物，这些药物在治疗癌症方面既温和又有效。异恶唑衍生物由于具有潜在的抗癌作用和最小的副作用，近年来受到了广泛关注。这些衍生物作为抗癌药物，具有不同的作用机制，如诱导细胞凋亡、芳香酶抑制、干扰微管聚集、拓扑异构酶抑制、组蛋白去乙酰化酶抑制和 ERα 抑制。在本文中，我们探讨了异恶唑衍生物的合成策略、抗癌作用机制以及构效关系研究。
