Pyrazole and Pyrazoline-Based EGFR TK Inhibitors: A Review Study Emphasizing Structure-Activity Relationship (SAR).

IF 1.9 4区 医学 Q3 CHEMISTRY, MEDICINAL
Shruti Mittal, Ozair Alam, Lakshay Singh, Kannan, Aasma Shakuli, Vishal Mathur, Mukund Jha, Anam Ilyas, Shaheen Ali, Mohd Javed Naim, Sana Tanweer
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引用次数: 0

Abstract

Unusual cell growth patterns, metastasis (the spread of tumors to other parts of the body), and potential death are all hallmarks of cancerResearch in oncology clearly shows that abnormalities in EGFR expression directly contribute to uncontrolled cell growth and division, resulting in the development of carcinomas.. People with cancer have developed resistance due to mutations in several EGFR-associated genes. Tyrosine kinase inhibitors (TKIs) and other cancer treatments must, therefore, undergo continuous improvement. Currently, fourth-generation tyrosine kinase inhibitors (TKIs) that act allosterically against the C797S mutation are the most widely used class of medications that target EGFR mutations. To help researchers better understand how to optimize pyrazole and pyrazoline-based derivatives as antiproliferative agents, this review summarises the work done in the last fifteen years on different anti-cancer agents representing 31 most potential compounds along with their activity characteristics, with a particular emphasis on the structure-activity relationship (SAR) of possible pyrazole and pyrazoline derivatives as EGFR tyrosine kinase inhibitors.

吡唑和吡唑啉类EGFR TK抑制剂:强调构效关系(SAR)的综述研究。
异常的细胞生长模式、转移(肿瘤扩散到身体其他部位)和潜在的死亡都是癌症的特征。肿瘤学研究清楚地表明,EGFR表达异常直接导致细胞生长和分裂失控,从而导致癌症的发展。由于几种egfr相关基因的突变,癌症患者产生了耐药性。因此,酪氨酸激酶抑制剂(TKIs)和其他癌症治疗必须不断改进。目前,第四代酪氨酸激酶抑制剂(TKIs)对C797S突变起变构作用,是针对EGFR突变使用最广泛的一类药物。为了帮助研究人员更好地了解如何优化吡唑和吡唑啉衍生物作为抗增殖药物,本文综述了近15年来对31种最有潜力的化合物及其活性特性的不同抗癌药物的研究,特别强调了吡唑和吡唑啉衍生物作为EGFR酪氨酸激酶抑制剂的构效关系(SAR)。
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
Medicinal Chemistry
Medicinal Chemistry 医学-医药化学
CiteScore
4.30
自引率
4.30%
发文量
109
审稿时长
12 months
期刊介绍: Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.
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