Pyrrole-based EGFR inhibitors for the treatment of NCSLC: Binding modes and SARs investigations

被引：6
作者：
He, Jie [1 ]
Luo, Leixuan [1 ]
Xu, Shidi [1 ]
Yang, Feiyi [1 ]
Zhu, Wufu [1 ]
机构：
[1] Jiangxi Sci & Technol Normal Univ, Sch Pharm, Jiangxi Prov Key Lab Drug Design & Evaluat, Nanchang, Jiangxi, Peoples R China
来源：
CHEMICAL BIOLOGY & DRUG DESIGN | 2023年 / 101卷 / 01期
基金：
中国国家自然科学基金;
关键词：
activity; molecular docking study; NSCLC; pyrrole; SAR; PAAL-KNORR SYNTHESIS; GUIDED DEVELOPMENT; MOLECULAR DOCKING; DUAL INHIBITORS; IN-VITRO; DERIVATIVES; DISCOVERY; DESIGN; POTENT; OSIMERTINIB;
D O I：
10.1111/cbdd.14169
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The treatment of advanced non-small cell lung cancer (NSCLC) has made substantial progress due to the rapid development of small molecule targeted therapy, with dramatically prolonged survival. As an effective drug for the treatment of NSCLC, epidermal growth factor receptor (EGFR) inhibitors are currently experiencing issues like severe adverse events and drug resistance. It is urgent to develop novel types of EGFR inhibitors to overcome the abovementioned limitations. Pyrrole always works well as a probe for the creation of novel medication candidates for hard-to-treat conditions like lung cancer. Although the design, synthesis, and biological assays of pyrrole derivatives have been reported, their inhibitory actions against the receptor tyrosine kinase (RTK) EGFR have not been in-depthly studied. This review highlights the small molecule EGFR inhibitors containing pyrrole heterocyclic pharmacophores in recent years, and the research on their mechanism, biological activity, and structure-activity relationship (SAR).
引用
收藏
页码：195 / 217
页数：23
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