三唑类作为生物电子等排体和连接子在微管靶向剂研发中的应用。
Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents.
作者信息
Malik M Shaheer, Ahmed Saleh A, Althagafi Ismail I, Ansari Mohammed Azam, Kamal Ahmed
机构信息
Department of Chemistry , Faculty of Applied Sciences , Umm Al-Qura University , 21955 Makkah , Saudi Arabia . Email:
Central Research Laboratories , Faculty of Applied Sciences , Umm Al-Qura University , 21955 Makkah , Saudi Arabia.
出版信息
RSC Med Chem. 2020 Jan 29;11(3):327-348. doi: 10.1039/c9md00458k. eCollection 2020 Mar 1.
Abstract
The triazole ring system has emerged as an exciting prospect in the optimization studies of promising lead molecules in the quest for new drugs for clinical usage. Several marketed drugs possess these versatile moieties that are used in a wide range of medical indications. This stems from the unique intrinsic properties of triazoles, which impart stability to the basic pharmacophoric unit with an added advantage of being a bioisostere of different chemical functionalities. In the last decade, the use of triazoles as bioisosteres and linkers in the development of microtubule targeting agents has been extensively investigated. The present review highlights the advances in this promising area of drug discovery and development.
摘要
在寻找临床应用新药的过程中，三唑环系统已成为有前景的先导分子优化研究中的一个令人兴奋的前景。几种上市药物含有这些多功能部分，用于广泛的医学适应症。这源于三唑独特的内在性质，它赋予基本药效基团稳定性，还有作为不同化学功能生物电子等排体的额外优势。在过去十年中，三唑作为生物电子等排体和连接子在微管靶向剂开发中的应用已得到广泛研究。本综述重点介绍了这一有前景的药物发现和开发领域的进展。
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