Article
Design, synthesis, and evaluation of pyrido.[3,4-b]pyrazin-2(1H)-one derivatives as potent FLT3 inhibitors.
Bioorganic & medicinal chemistry - 1 Feb 2023
Sun Mei, Wang Chang, Wang Peipei, Ye Qingqing, Zhou Yubo, Li Jia, Liu Tao
Abstract excerpt
Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as driver mutations in a subgroup of AML patients. Herein, we describe the design, synthesis, and biological evaluation of a novel series of potent pyrido.[3,4-b]pyrazin-2(1H)-one derivatives as FLT3 inhibitors. The compounds exhibited...
Topics
- Animals
- Mice
- Antineoplastic Agents
- Apoptosis
- Cell Line, Tumor
- Cell Proliferation
- fms-Like Tyrosine Kinase 3
- Leukemia, Myeloid, Acute
- Microsomes, Liver
- Mutation
- Protein Kinase Inhibitors