Jaballah Maiy Youssef, Serya Rabah Taha, Abouzid Khaled
Faculty of Pharmacy, Pharmaceutical Chemistry Department, Ain Shams University, Cairo, Egypt.
Drug Res (Stuttg). 2017 Mar;67(3):138-148. doi: 10.1055/s-0042-119992. Epub 2017 Jan 10.
Pyridazines, their oxo derivatives; pyridazinone as well as fused bi- or tricyclic pyridazine containing scaffolds are key structural features of many biologically active compounds with diverse pharmacological applications, including cancer therapy. Since protein kinases play prominent role in tumor biology, the inhibition of its signaling pathway is considered an effective therapeutic option for the treatment of cancer.Based on the various advantages of pyridazines in drug design including modulation of the physico-chemical properties, improving ADME and toxicity profile as well as easy and diverse synthetic methods of access, makes them an invaluable tool for designing compounds as future drugs for targeted cancer treatment.In this review, we have compiled and discussed the anticancer potential of pyridazine based scaffold, with special focus on those targeting protein kinase inhibition.
哒嗪及其氧代衍生物；哒嗪酮以及含有哒嗪骨架的稠合双环或三环结构是许多具有多种药理应用（包括癌症治疗）的生物活性化合物的关键结构特征。由于蛋白激酶在肿瘤生物学中发挥着重要作用，抑制其信号通路被认为是治疗癌症的一种有效治疗选择。基于哒嗪在药物设计中的各种优势，包括调节物理化学性质、改善药物代谢动力学和毒性特征以及简便多样的合成方法，使其成为设计未来靶向癌症治疗药物的宝贵工具。在本综述中，我们汇编并讨论了基于哒嗪骨架的抗癌潜力，特别关注那些靶向蛋白激酶抑制的化合物。
