Small molecule compound and its application in preparing medicine for treating FLT3 mutant leukemia

• Main Authors: DU Jiahui, WANG Jun, XUE Shengli, LIU Songbai, QIU Qiaocheng, GE Shuaishuai, DAI Haiping
• Format: Patent
• Language: English
• Published: 05.12.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

The invention discloses a small molecular compound and its application in preparing a medicine for treating FLT3 mutant leukemia, belonging to the field of biomedicine. The micromolecule compound drug 17 is a micromolecule compound designed by screening the binding sites of wild-type and mutant FLT3 activated state structural models based on homologous molecular models. Experiments show that drug 17 can inhibit the growth of FLT3-ITD mutant leukemia cells, inhibit the phosphorylation level of FLT3, promote cell apoptosis and lead to cycle arrest in vitro. Moreover, at the biochemical level, drug 17 can inhibit the activity of FLT3 protein kinase to a certain extent, and the IC50 can reach the micromolar level. The micromolecule compound drug 17 provided by the invention is expected to reduce the drug resistance problem of secondary TKD region mutation, and provides new hope for accurate targeted treatment of AML patients with FLT3 mutation.