Cancer is one of the main causes of death throughout the world. The anticancer agents are indispensable for the treatment of various cancers, but most of them currently on the market are not specific, resulting in series of side effects of chemotherapy. Moreover, the emergency of drug-resistance towards cancers has already increased up to alarming level in the recent decades. Therefore, it's imperative to develop novel anticancer candidates with excellent activity against both drug-susceptible and drug-resistant cancers, and low toxicity as well. Tetrazole is the bioisoster of carboxylic acid, and its derivatives demonstrated promising anticancer activity. Hybridization of tetrazole with other anticancer pharmacophores may provide novel candidates with anticancer potency. The present review described the anticancer activity of tetrazole hybrids, and the structure-activity relationship (SAR) is also discussed to provide an insight for rational designs of tetrazole anticancer candidates with higher efficiency.

癌症是全世界死亡的主要原因之一。抗癌剂对于治疗各种癌症是必不可少的，但是目前市场上的大多数抗癌剂都不是特异性的，从而导致一系列化学疗法的副作用。此外，在最近几十年中，对癌症的耐药性紧急情况已经上升到令人震惊的水平。因此，迫切需要开发出对药物敏感性和耐药性都具有优异活性且毒性低的新型抗癌候选药物。四唑是羧酸的生物等排体，其衍生物显示出有希望的抗癌活性。四唑与其他抗癌药效基团的杂交可提供具有抗癌效力的新型候选物。