Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Mini Rev Med Chem. 2023;23(17):1733-1759. doi: 10.2174/1389557523666230201113237.
Cancer is one of the severe diseases in which abnormal cells divide and proliferate in an uncontrolled manner without any regulation. Globally cancer is among the leading causes of death; according to a recent report of by the WHO, around 10 million people died in 2018 due to cancer. It has also been reported that by 2040, approximately 30 million new cases will be reported every year. The increase in the incidences of cancer is taking a toll on the health care system worldwide. Considerable scientific literature is available on anticancer agents but newer therapeutic strategies are still required in this field to address novel approaches to drug design and discovery to counter this problem. Imidazothiazole represents a privileged scaffold in medicinal chemistry and provides the medicinal chemist the possibility to modulate the physiochemical properties of the lead compound. In recent times, imidazothiazole scaffold is broadly explored for its anticancer activity, which acts through various mechanisms such as EGFR, B-RAF, DHFR kinase inhibition and tubulin polymerization inhibition and other molecular mechanisms of action. Due to their feasible synthetic accessibility and promising pharmacological profile, it has attracted various medicinal chemists to explore and develop imidazothiazole derivatives as potent and safe anticancer agents. In the present article, we have reviewed various potent imidazothiazole scaffold-based derivatives reported as anticancer agents, their synthetic strategies, Structure Activity Relationship (SAR), mechanism of action, and molecular docking along with their future perspective. This review will be very useful for medicinal chemists for drug design and development of imidazothiazole-based potent antiproliferative agents.
癌症是一种严重的疾病，其中异常细胞不受控制地分裂和增殖，没有任何调节。在全球范围内，癌症是导致死亡的主要原因之一；根据世界卫生组织最近的一份报告，2018 年约有 1000 万人死于癌症。据报道，到 2040 年，每年将报告约 3000 万例新病例。癌症发病率的增加正在给全球医疗保健系统带来压力。有大量关于抗癌药物的科学文献，但在该领域仍需要新的治疗策略，以解决药物设计和发现的新方法，以应对这一问题。咪唑并噻唑代表了药物化学中的一个特权支架，并为药物化学家提供了调节先导化合物的物理化学性质的可能性。在最近的一段时间里，咪唑并噻唑支架因其抗癌活性而被广泛探索，它通过多种机制发挥作用，如 EGFR、B-RAF、DHFR 激酶抑制和微管蛋白聚合抑制以及其他作用机制。由于其可行的合成可及性和有希望的药理学特性，它吸引了许多药物化学家探索和开发咪唑并噻唑衍生物作为有效的和安全的抗癌药物。在本文中，我们综述了各种报道的作为抗癌药物的基于咪唑并噻唑支架的有效衍生物，及其合成策略、构效关系（SAR）、作用机制、分子对接以及它们的未来前景。这篇综述对药物化学家设计和开发基于咪唑并噻唑的有效的抗增殖剂药物将非常有用。
