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作为具有抗微生物活性的抗癌剂的基于pyridazinone的衍生物:分子设计,合成和生物研究

Mohamed K S El-Nagar¹, Mai I Shahin², Mohammed F El-Behairy¹

¹Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City Sadat City Menoufia 32897 Egypt.

RSC medicinal chemistry

|September 9, 2024

概括

这项研究开发了新的基于化的二甲基尿素化合物,具有抗癌和抗菌性质. 这些药物在对抗感染和抑制癌细胞生长方面表现有前途,为癌症患者提供了双重治疗方法.

科学领域:

药用化学医学化学
药理学药理学是指药理学的学科.
在瘤学瘤学.

背景情况:

化疗患者面临感染风险增加和由炎症驱动的癌症进展.
需要新型药物,具有结合抗癌和抗菌作用.

研究的目的:

设计和合成基于化的新型二甲基尿素衍生物.
评估这些化合物的双重抗癌和抗微生物活性.
为了确定索拉费尼布的潜在替代品,以改善治疗概况.

主要方法:

尿素衍生物的合成和表征.
对黄金葡萄球菌和白菌的抗菌活性测试.
通过国家癌症研究所 (NCI) 对60个癌症细胞系进行抗癌查.
VEGFR-2 抑制测定和分子对接研究.
细胞周期分析和基因表达概况 (p53,Bax,Bcl-2).

主要成果:

化合物10h和8g分别表现出强大的抗菌和抗真菌活性.
化合物17a显示出显著的VEGFR-2抑制活性.
化合物8f,10l和17a表现出广泛的抗癌活性 (62.21%-100.14%GI%).
化合物10l诱导了G0-G1细胞周期停止和调节的亡相关基因表达.
分子对接支持化合物与VEGFR-2的结合.

结论:

基于pyridazinone的腹尿素衍生物具有双重的抗微生物和抗癌潜力.
这些化合物是作为新型化疗剂进一步开发的有希望的候选物.
这些发现支持治疗易受感染的癌症患者的新策略.

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