Non-fused Pyrimidine Derivatives as Potential Pharmacological Entities: A Review.

IF 2.9 4区医学 Q3 CHEMISTRY, MEDICINAL

Current topics in medicinal chemistry Pub Date : 2024-10-09 DOI:10.2174/0115680266317088240924205745

Khyati L Bharti, Parnas S Parmar, Bhavesh P Rathod, Sharmil N Anjirwala, Saurabh K Patel

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引用次数: 0

Abstract

Non-fused pyrimidine scaffold is a significant component for designing new drugs. The review emphasizes the pharmacological importance of non-fused pyrimidine-containing moieties based on the broad spectrum of activities such as antiprotozoal, antibacterial, antimycobacterial, anticancer, anti-inflammatory activity, and CNS depressant. Pyrimidine derivatives are fascinating entities that display biological activities for the treatment of cancer. It also highlights the tendency of non-fused pyrimidine derivatives to suppress cell growth by obstructing the activity of VCP, CDK-2, EGFR, ATR, EphB4 & EphA2, PDGF as well as inhibitory action towards different cell lines such as MCF-7, HeLa, NCI/ADR-RES, NCIH23, HOP-92, HCT-116, OV-3, MOLT-4, PC-3, MDA-MB-231, MALME-3M, K562 and Bcr-Abl. The review details the importance of morpholine, piperidine, and pyrrolidine ring substitutions on pyrimidine moiety as well as the role of H-bonding and amino linkage along with antibacterial activity due to the presence of pleuromutilin and tetrazole molecules. Researchers were motivated to develop and enhance the non-fused pyrimidine scaffold to uncover novel medicines by reading this review article.

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作为潜在药理实体的非融合嘧啶衍生物：综述。

非融合嘧啶支架是设计新药物的重要组成部分。这篇综述基于抗原虫、抗菌、抗霉菌、抗癌、抗炎和中枢神经系统抑制剂等广泛的活性，强调了含非融合嘧啶分子的药理学重要性。嘧啶衍生物是令人着迷的实体，具有治疗癌症的生物活性。它还突出了非融合嘧啶衍生物通过阻碍 VCP、CDK-2、表皮生长因子受体、ATR、EphB4 和 EphA2 的活性来抑制细胞生长的趋势、PDGF 以及对不同细胞系的抑制作用，如 MCF-7、HeLa、NCI/ADR-RES、NCIH23、HOP-92、HCT-116、OV-3、MOLT-4、PC-3、MDA-MB-231、MALME-3M、K562 和 Bcr-Abl。综述详细介绍了嘧啶分子上吗啉、哌啶和吡咯烷环取代的重要性，以及 H 键和氨基连接的作用，以及由于褶菌林和四唑分子的存在而产生的抗菌活性。通过阅读这篇综述文章，激发了研究人员开发和改进非融合嘧啶支架以开发新型药物的兴趣。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current topics in medicinal chemistry 医学-医药化学

CiteScore

6.40

自引率

2.90%

发文量

186

审稿时长

3-8 weeks

期刊介绍： Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.