Work

Dual FLT3/haspin kinase inhibitor based on 3 H -pyrazolo[4,3- f ]quinoline scaffold with activities against acute myeloid leukemia

Year: 2023

Type: article

Abstract: values between 2-25 nM. Western blot analyses of treated AML cells confirm that HSK205 inhibit the phosphorylation of both FLT3 and histone H3 (a haspin target) in cells. While multi-component reactions (MCRs) have been used to make many bioactive molecules, there are very few examples of using MCRs to make compounds that target protein kinases, which have emerged as one of the top drug candidates (especially in oncology). This work highlights our recent efforts to make ultrapotent protein kinase inhibitors using multi-component reactions (especially the Doebner-Povarov reaction).

Source: RSC Medicinal Chemistry

DOI: 10.1039/d3md00192j

Authors: Allison L. Kempen, Nickolas R. Brauer, Herman O. Sintim

Institutions: Purdue University West Lafayette, Purdue University Institute for Cancer Research

Language: English

Topic: Heterocyclic Compound Synthesis and Bioactivity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: bronze

Funders: Foundation for the National Institutes of Health, Purdue University, National Institutes of Health, National Cancer Institute