sp2/sp3杂化在C-3取代的含吲哚先导分子和FDA批准药物的药用意义

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL
Mohd Faiyyaz, Akanksha Tiwari, Nuzhat Bashir, Malik Nasibullah, Sahir Sultan Alvi, Mohammed Haris Siddiqui, Mohd Asif
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引用次数: 0

摘要

本文总结了与半合成和从天然资源中提取的含吲哚支架有关的具有生物学重要性的特权。此类化合物已显示出显著的药用价值,并经美国食品药物管理局批准用于治疗各种癌症。吲哚骨架衍生物的化学性质表明,当它们与极性溶剂接触时,在特定条件下会出现各种构象,包括同分异构;因此,这些现象是增强酶的生物效应的原因。在过去十年的上述综述研究中,我们证明了共振结构的生物学意义和药物分析的转变。我们注意到,π键-不饱和官能团、sp1/2/3杂化亚甲基、环醚、伯氨基、卤素和交错构象显示出最有效的活性药物样分子。本报告的目的是,今后可根据药物类先导分子表面可能存在的活性位点对其进行衍生,以发现更有效的药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Medicinal significance of sp2/sp3 hybridized at C-3-substituted indole-containing lead molecules and FDA-approved drugs

Medicinal significance of sp2/sp3 hybridized at C-3-substituted indole-containing lead molecules and FDA-approved drugs

Herein, the privilege in favor of biological importance of indole-containing scaffolds related to the semi-synthetic and extracted from natural sources is summarized. Such compounds have shown notable medicinal significance and are used in the treatment of various carcinomas after FDA approval. The chemistry of indoles’ skeleton derivatives showed various conformations at specific conditions, including tautomerization, when they came into contact with polar solvents; consequently, such phenomena are responsible for enhancing the biological effect on enzymes. In the foregoing review study in the past decade, we demonstrated the biological significance and the transformation of drug analysis owing to resonating structures. Functionalize groups, it was noted that pi-bonds-unsaturated functions, sp1/2/3 hybridized methylene groups, cyclic ethers, primary amino groups, halogens, and staggered conformations displayed the most potent active drug-like molecules. The aim of this report is that drugs like lead molecules could be derivatized for the discovery of more effective drugs on the basis of their possible active sites on the surface in the future.

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来源期刊
Medicinal Chemistry Research
Medicinal Chemistry Research 医学-医药化学
CiteScore
4.70
自引率
3.80%
发文量
162
审稿时长
5.0 months
期刊介绍: Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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