Shruti Mittal, Ozair Alam, Lakshay Singh, Kannan, Aasma Shakuli, Vishal Mathur, Mukund Jha, Anam Ilyas, Shaheen Ali, Mohd Javed Naim, Sana Tanweer
{"title":"Pyrazole and Pyrazoline-Based EGFR TK Inhibitors: A Review Study Emphasizing Structure-Activity Relationship (SAR).","authors":"Shruti Mittal, Ozair Alam, Lakshay Singh, Kannan, Aasma Shakuli, Vishal Mathur, Mukund Jha, Anam Ilyas, Shaheen Ali, Mohd Javed Naim, Sana Tanweer","doi":"10.2174/0115734064373755250409165138","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":1.9000,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115734064373755250409165138","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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.
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.