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具有抗血管遗传性质的新型5-氨基醇:设计,合成和生物评估
Matteo Lusardi1, Bernhard Wehrle-Haller2, Adama Sidibe2
1Department of Pharmacy, Section of Medicinal Chemistry, Università degli Studi di Genova, Viale Benedetto XV 3, I-16132, Genova, Italy.
European journal of medicinal chemistry
|August 19, 2023
概括
合成了新型的5 - 氨基醇,并发现它们具有非细胞毒性. 这些化合物有效地抑制了Akt酸化,并影响细胞迁移,显示出抗血管生成疗法的潜力.
科学领域:
- 药用化学 医学化学
- 分子生物学分子生物学
- 细胞生物学 细胞生物学
背景情况:
- 之前合成的醇尿酸表现出抗血管新生性质.
- 这项研究侧重于具有多种pyrazole核装饰的新型5-aminopyrazoles.
研究的目的:
- 合成和描述新型的5 - 氨基醇.
- 评估这些化合物的细胞毒性和抗血管性潜力.
- 研究它们对MAPK和PI3K信号通路的影响.
主要方法:
- 合成5-阿米诺皮拉醇 (化合物2-5).
- 使用MTT测定对瘤细胞系和纤维细胞的细胞毒性评估.
- 在人类前皮纤维细胞 (HFF) 和人类静脉内皮细胞 (HUVEC) 上进行EDU增殖测定.
- 对ERK1/2和Akt酸化的西部斑点分析.
- 伤口愈合测试以评估细胞迁移.
主要成果:
- 所有合成的pyrazole衍生品 (2-5) 在20μM以下是非细胞毒性的.
- 化合物3b和3c显著抑制了HFF和HUVEC细胞中的Akt酸化.
- 衍生品2和3在伤口愈合试验中显示出对HFF细胞迁移的强烈影响.
结论:
- 新型5-aminopyrazoles是非细胞毒性的,并具有抗血管生成性质.
- 特定的衍生物显示出抑制病态细胞迁移和血管生成的潜力.
- 这一化学品类对开发新疗法剂具有吸引力.
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