带有细胞毒性活性的酸衍生物 - - 综述
Georgi Tirolski1, Georgi Momekov2, Emiliya Cherneva3
1Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, Dunav -2 Street, 1000, Sofia, Bulgaria; Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Build. 9, 1113, Sofia, Bulgaria.
Chemico-biological interactions
|December 8, 2024
概括
酸衍生物通过破坏癌细胞离子梯度,抑制瘤生长酶,并作为放射性药物中的链接剂,显示出显著的抗癌潜力. 这些化合物对包括结直肠癌和乳腺癌在内的各种癌症类型表现出强烈的活性.
科学领域:
- 药用化学 医学化学
- 在瘤学瘤学.
- 药物发现 药物发现 药物发现
背景情况:
- 酸 (SQ) 衍生物是由于其独特的平面芳香环,结合能力和反应性而是一种有前途的药物剂类.
- 它们与碳酸盐,酸盐和胺基团的结构相似性增强了它们的类似药物的特性.
研究的目的:
- 本综述提供了对酸衍生物在抗癌疗法中的潜在应用的首次全面分析.
- 它检查了2000年至2024年间发表的实验研究,以评估它们对各种癌症的疗效.
主要方法:
- 该评论分析了体外研究,证明了酸衍生物的抗癌活性.
- 它还考虑了在固体瘤的II期临床试验中对酸衍生物Navarixin的评估.
主要成果:
- 化方胺作为离子载体,破坏癌细胞离子梯度并诱导亡.
- 酸衍生物被确定为选择性抑制酶,如HDACs,FAK和酶参与瘤进展.
- 环二的部分作为一个有效的链接器在放射性药物用于癌症治疗.
结论:
- 酸衍生物具有强大的体外抗癌活性,一些化合物在纳米分子范围内对各种癌症细胞系表现出有效性.
- 它们的多方面的机制,包括离子运输中断,酶抑制和治疗应用,突出显示了它们的治疗前景.
- 正在进行进一步的临床评估,例如Navarixin,这凸显了这些化合物的在瘤学中的翻译潜力.
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