Identification of potent anticancer agents with high selectivity and low toxicity remains on the way to human health. Pyridazine featuring advantageous physicochemical properties and antitumor potential usually is regarded as a central core in numerous anticancer derivatives. There are several approved pyridazine-based drugs in the market and analogues currently going through different clinical phases or registration statuses, suggesting pyridazine as a promising drug-like scaffold. The current review is intended to provide a comprehensive and updated overview of pyridazine derivatives as potential anticancer agents. In particular, we focused on their structure-activity relationship (SAR) studies, design strategies, binding modes and biological activities in the hope of offering novel insights for further rational design of more active and less toxic anticancer drugs.

具有高选择性和低毒性的有效抗癌药的鉴定仍在通往人类健康的道路上。哒嗪具有良好的理化性质和抗肿瘤潜力，通常被认为是众多抗癌衍生物的核心。市场上有几种批准的基于哒嗪的药物，其类似物目前正经历不同的临床阶段或注册状态，这表明哒嗪是一种很有前途的药物样支架。本综述旨在提供哒嗪衍生物作为潜在抗癌药的全面更新的概述。特别是，我们专注于他们的结构-活性关系（SAR）研究，设计策略，