HDAC 抑制剂的发现与开发:癌症治疗方法小综述》。

Roshani Patel, Arjun Modi, Hitesh Vekariya
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引用次数: 0

摘要

组蛋白去乙酰化酶(HDAC)抑制剂能够诱导癌细胞分化、细胞周期停滞和凋亡,因此已成为很有前景的癌症治疗药物。在本综述中,我们介绍了 HDAC 抑制剂的系统发现和开发。全球的研究人员已经发现了多种小分子药物,如苯并[d][1,3]二恶茂衍生物、贝利诺司他类似物、吡嗪衍生物、喹唑啉- 4-酮基衍生物、2,4-咪唑二酮衍生物、吖啶羟肟酸衍生物、香豆素衍生物、四氢呋喃衍生物、苯并[d][1,3]二恶茂衍生物等、香豆素衍生物、四氢异喹啉衍生物、噻唑-5-甲酰胺、水杨酰胺衍生物、β-肽封端 HDAC 抑制剂、喹唑啉衍生物、苯并咪唑和苯并噻唑衍生物,以及含有 HDAC 抑制剂的β-榄香烯支架。大多数支架在各种细胞系(如 HDAC1、HDAC2、HDAC6、PI3K、HeLa、MDA-MB-231、MCF-10A、MCF-7、U937、K562 和 Bcr-Abl 细胞系)中显示出诱人的 IC50 (μM)。
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Discovery and Development of HDAC Inhibitors: Approaches for the Treatment of Cancer a Mini-review.

Histone deacetylase (HDAC) inhibitors have emerged as promising cancer therapeutics due to their ability to induce differentiation, cell cycle arrest, and apoptosis in cancer cells. In the present review, we have described the systemic discovery and development of HDAC inhibitors. Researchers across the globe have identified various small molecules like benzo[d][1,3]dioxol derivatives, belinostat analogs, pyrazine derivatives, quinazolin-4-one-based derivatives, 2,4-imidazolinedione derivatives, acridine hydroxamic acid derivatives, coumarin derivatives, tetrahydroisoquinoline derivatives, thiazole-5-carboxamide, salicylamide derivatives, β-peptoid-capped HDAC inhibitors, quinazoline derivatives, benzimidazole and benzothiazole derivatives, and β- elemene scaffold containing HDAC inhibitors. Most of the scaffolds have shown attractive IC50 (μM) in various cell lines like HDAC1, HDAC2, HDAC6, PI3K, HeLa, MDA-MB-231, MCF-10A, MCF-7, U937, K562 and Bcr-Abl cell lines.

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