Cancer is a leading cause of death worldwide. Even after the availability of numerous drugs and treatments in the market, scientists and researchers are focusing on new therapies because of their resistance and toxicity issues. The newly synthesized drug candidates are able to demonstrate in vitro activity but are unable to reach clinical trials due to their rapid metabolism and low bioavailability. Therefore there is an imperative requisite to expand novel anticancer negotiators with tremendous activity as well as in vivo efficacy. Tetrazole is a promising pharmacophore which is metabolically more stable and acts as a bioisosteric analogue for many functional groups. Tetrazole fragment is often castoff with other pharmacophores in the expansion of novel anticancer drugs. This is the first systematic review that emphasizes on contemporary strategies used for the inclusion of tetrazole moiety, mechanistic targets along with comprehensive structural activity relationship studies to provide perspective into the rational design of high-efficiency tetrazole-based anticancer drug candidates.

癌症是全球主要的死亡原因。即使在市场上获得了众多药物和疗法之后，由于其抗药性和毒性问题，科学家和研究人员仍将重点放在新疗法上。新合成的候选药物能够表现出体外活性，但由于其快速代谢和低生物利用度而无法进行临床试验。因此，迫切需要扩展具有巨大活性以及在体内的新型抗癌谈判者。功效。四唑是一种有前途的药效基团，在代谢上更稳定，并可以作为许多官能团的生物立体异构体。在新型抗癌药物的扩展中，四唑片段通常会与其他药效团分离。这是第一个系统综述，重点介绍了当代策略，包括四唑部分的使用，机理靶标以及全面的结构活性关系研究，从而为基于四唑的高效抗癌候选药物的合理设计提供了视角。