Chandigarh College of Pharmacy, Landran, Punjab, India.
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
Anticancer Agents Med Chem. 2020;20(18):2228-2245. doi: 10.2174/1871520620666200807220146.
Phthalazinones are important nitrogen-rich heterocyclic compounds which have been a topic of considerable medicinal interest because of their diversified pharmacological activities. This versatile scaffold forms a common structural feature for many bioactive compounds, which leads to the design and development of novel anticancer drugs with fruitful results. The current review article discusses the progressive development of novel phthalazinone analogues that are targets for various receptors such as PARP, EGFR, VEGFR-2, Aurora kinase, Proteasome, Hedgehog pathway, DNA topoisomerase and P-glycoprotein. It describes mechanistic insights into the anticancer properties of phthalazinone derivatives and also highlights various simple and economical techniques for the synthesis of phthalazinones.
酞嗪酮是一类重要的含氮杂环化合物，由于其多样化的药理活性，一直是医学领域的研究热点。这种多功能的结构骨架是许多生物活性化合物的共同结构特征，这导致了新型抗癌药物的设计和开发，并取得了丰硕的成果。本文综述了新型酞嗪酮类似物的研究进展，这些类似物是各种受体的靶点，如 PARP、EGFR、VEGFR-2、Aurora 激酶、蛋白酶体、Hedgehog 通路、DNA 拓扑异构酶和 P-糖蛋白。本文描述了酞嗪酮衍生物的抗癌特性的作用机制，并强调了各种简单经济的酞嗪酮合成技术。
