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Review Article

临床认可的蛋白激酶抑制剂的结构-性质关系

卷 30, 期 22, 2023

发表于: 24 October, 2022

页: [2518 - 2541] 页: 24

弟呕挨: 10.2174/0929867329666220822123552

价格: $65

摘要

背景：在过去几十年中，蛋白激酶抑制剂已成为最成功的小分子药物类别之一。在现代药物发现中，在药物设计中尽早考虑“类药”物理化学和药代动力学特性被广泛认为是降低药物损耗率的重要策略。 方法：在这篇综述中，比较了临床批准的 25 种蛋白激酶抑制剂及其在药物化学文献中报道的关键类似物的生物学、物理化学和药代动力学特性。尽管在复杂的药物发现活动中没有共同的轨迹可以遵循，但从成功的先导优化研究中获得的结构-活性关系的知识可能会扩展到其他药物设计工作。 结果：在全球临床批准的 70 多种蛋白激酶抑制剂中，25 种抑制剂及其关键类似物的结构-活性关系是从药物化学文献中汇编的，其中“先导到候选”阶段的详细结果与相关联财产数据。对于其他抑制剂，此类信息尚未在文献中公开，或者可用数据有限且不足以提供清晰的结构分析。 结论：总结了 25 种抑制剂及其类似物的结构-性质关系，说明了先导化合物优化和候选药物选择的一般准则，并且可以扩展此信息以用于将来更好的基于性质的药物设计。

关键词: 结构-性质关系、蛋白激酶抑制剂、增溶基团、先导物优化、候选药物选择、药物发现。

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