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探索4,7-不替代的Pyrimido[4,5-d]pyrimidines作为抗病毒和抗癌剂

Eleftheria A Georgiou¹, Konstantinos Paraskevas¹, Christina Koutra²

¹Department of Pharmacy, Division of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece.

Molecules (Basel, Switzerland)

|December 17, 2024

概括

新的pyrimido[4,5-d]pyrimidine化合物显示出作为抗癌和抗病毒剂的承诺. 衍生品证明了对血液癌症和人类冠状病毒229E (HCoV-229E) 的有效性,这表明药物开发的潜力.

科学领域:

药用化学医学化学
有机合成有机合成
病毒学病毒学

背景情况:

皮里米多[4,5-d]皮里米丁基架因其生物活动而闻名.
开发用于癌症和病毒感染的新疗法仍然是全球卫生优先事项.

研究的目的:

为了合成新型的4,7-非替代的pyrimido[4,5-d]pyrimidine衍生物.
评估这些合成化合物的抗增殖和抗病毒活性.

主要方法:

从thiourea开始,采用了一种简单的合成方法.
对八个癌症细胞系进行了抗增殖活性评估.
对一组病毒进行抗病毒功效评估,包括人类冠状病毒229E (HCoV-229E).

主要成果:

成功合成了13种新的pyrimido[4,5-d]pyrimidine衍生物.
化合物7d和7h对血液癌症类型表现出显著的抗增殖作用.
含有环烯胺和氨基胺部分的化合物对HCoV-229E.表现出显著的疗效.

结论:

皮里米多[4,5-d]皮里米丁支架是开发针对HCoVs的新抗病毒药物的有希望的框架.
化合物7a,7b和7f被确定为进一步研究和开发的强有力的候选者,作为HCoV-229E抗病毒药物.

关键词:

人类新冠病毒-229E 反扩散活动的反扩散活动.抗病毒活动的抗病毒活性.皮里米多[4,5-d] 皮里米丁综合合成是一种合成.

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