C5-substituted pyrido[2,3-d]pyrimidin-7-ones as highly specific kinase inhibitors targeting the clinical resistance-related EGFRT790M mutant

Author:

Xu Tianfeng12345,Peng Ting67385,Ren Xiaomei12345,Zhang Lianwen12345,Yu Lei12345,Luo Jinfeng12345,Zhang Zhang12345,Tu Zhengchao12345,Tong Linjiang67385,Huang Zhaoru67385,Lu Xiaoyun12345,Geng Meiyu67385,Xie Hua67385,Ding Jian67385,Ding Ke12345

Affiliation:

1. State Key Laboratory of Respiratory Diseases

2. Guangzhou Institute of Biomedicine and Health

3. Chinese Academy of Sciences

4. Guangzhou 510530

5. China

6. State Key Laboratory of Drug Research

7. Shanghai Institute of Materia Medica

8. Shanghai 201203

Abstract

C5-substituted pyrido[2,3-d]pyrimidin-7-ones were discovered as highly potent and specific inhibitors targeting the clinical resistance-related EGFRL858R/T790M mutant.

Funder

National Natural Science Foundation of China

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

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