Background: Colorectal cancer is the third foremost cause of death in women and men. Globally, about 1.94 million colon cancer cases were diagnosed and around 0.93 million patients died in the previous year. Introduction: Several drugs have been permitted by the Food And Drug Administration (FDA) for the treatment of colorectal cancer. The main difficulties of current drugs are the expansion of resistance issues, target selectivity issues and toxicity issues. The existing therapies, such as surgery and hormonal therapy, are in use but exhibit numerous adverse effects, such as pharmacokinetic issues and pharmacodynamic issues. Hence, hereby is a crucial requirement of novel moieties that are peaceable and efficient in the handling of colorectal cancer. Method: Phthalazine derivatives have expanded admiration over a few years due to their efficient anticancer significance. These Phthalazine derivatives exhibit anticancer activity by targeting various mechanisms such as apoptosis induction, tubulin polymerization inhibition, EGFR inhibition, and aurora kinase inhibition. Result: In this study, we have focused on the Structural Activity relationship, numerous synthetic strategies and mechanism of action of phthalazine derivatives for potential treatment of cancer. Conclusion: Among some of phthalazine derivative compounds not only induced antiproliferative activity even also improved bioavailability and reduced side effects, like 4-(phthalazine-1-yl) aniline with (IC50 = 0.22 ± 0.11 μM), and 4-phthalazin-1-yl-amino) benzonitrile (IC50 = 1.20 μM), 4-((5- methyl-pyrazole-3-yl) amino)-2-phenylphthalazin-1-one (IC50 = 0.031 μM) and 4-((5-methylpyrazole- 3-yl) amino)-2-(p-tolyl)phthalazin-1-one (IC50 = 0.065 μM). Therefore, this study would be the inspiration for the betterment of human health.

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酞嗪衍生物抗癌剂的合成策略、作用机制及SAR研究简述

背景：结直肠癌是女性和男性死亡的第三大原因。去年，全球约有 194 万结肠癌确诊病例，约 93 万患者死亡。简介：美国食品和药物管理局 (FDA) 已批准多种药物用于治疗结直肠癌。目前药物的主要难点是耐药性扩大问题、靶点选择性问题和毒性问题。现有的疗法，例如手术和激素疗法，正在使用，但表现出许多副作用，例如药代动力学问题和药效学问题。因此，这是对在结直肠癌治疗中和平且有效的新型部分的关键要求。方法：近年来，酞嗪衍生物因其有效的抗癌作用而受到广泛关注。这些酞嗪衍生物通过靶向多种机制（例如细胞凋亡诱导、微管蛋白聚合抑制、EGFR 抑制和极光激酶抑制）表现出抗癌活性。结果：在这项研究中，我们重点研究了二氮杂萘衍生物的结构活性关系、众多合成策略和作用机制，用于潜在的癌症治疗。结论：一些二氮杂萘衍生化合物不仅具有抗增殖活性，还提高了生物利用度并减少了副作用，例如 4-(二氮杂萘-1-基)苯胺 (IC50 = 0.22 ± 0.11 μM) 和 4-二氮杂氮-1-基-氨基)苯甲腈 (IC50 = 1.20 μM)、4-((5-甲基-吡唑-3-基)氨基)-2-苯基酞嗪-1-酮 (IC50 = 0.031 μM) 和 4-((5-甲基吡唑) - 3-基)氨基)-2-(对甲苯基)酞嗪-1-酮 (IC50 = 0.065 μM)。因此，这项研究将为改善人类健康带来启发。