Structure-Based Optimization of Pyrazinamide-Containing Macrocyclic Derivatives as Fms-like Tyrosine Kinase 3 (FLT3) Inhibitors to Overcome Clinical Mutations

Author:

Zheng Xuan1,Chen Zhiwen1,Guo Ming2ORCID,Liang Hong1,Song Xiaojuan1,Liu Yiling1,Liao Zhenling1,Zhang Yan1,Guo Jing1,Zhou Yang1ORCID,Zhang Zhi-min1,Tu Zhengchao1,Zhang Ye3,Chen Yongheng2ORCID,Zhang Zhang1ORCID,Lu Xiaoyun14ORCID

Affiliation:

1. State Key Laboratory of Bioactive Molecules and Druggability Assessment, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education, Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, #855 Xingye Avenue, Guangzhou 510632, China

2. Department of Oncology, NHC Key Laboratory of Cancer Proteomics, State Local Joint Engineering Laboratory for Anticancer Drugs, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China

3. Guangxi Key Laboratory of Drug Discovery and Optimization, School of Pharmacy, Guilin Medical University, Guilin 541199, China

4. Department of Hematology, Guangdong Second Provincial General Hospital, Jinan University, Guangzhou 510632, China

Funder

Natural Science Foundation of Hunan Province

Basic and Applied Basic Research Foundation of Guangdong Province

Guilin Medical University

Jinan University

National Natural Science Foundation of China

Guangdong Provincial Key Laboratory of New Drug Design and Evaluation

Guangxi Key Laboratory of Drug Discovery and Optimization

Publisher

American Chemical Society (ACS)

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