1H-Pyrazole-3-acetamide, 5-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-

AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.

AZD-1152 is a member of the of quinazolines that is 4-aminoquinazolin-7-ol in which the amino group at position 4 has been substituted by a 5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl group, while the hydroxy group at position 7 has been converted into the corresponding 3-[ethyl(2-hydroxyethyl)aminopropyl ether. It has a role as an antineoplastic agent and an Aurora kinase inhibitor. It is a member of quinazolines, a secondary carboxamide, a tertiary amino compound, a secondary amino compound, a member of pyrazoles, a primary alcohol, a member of monofluorobenzenes and an anilide.|Defosbarasertib is a small-molecule inhibitor of the serine-threonine kinase Aurora B, with potential antineoplastic activity. Upon administration, defosbarasertib specifically binds to and inhibits Aurora kinase B, which disrupts spindle checkpoint functions and chromosome alignment, and results in the disruption of chromosome segregation and cytokinesis. This inhibits cell division and cell proliferation and induces apoptosis in Aurora kinase B-overexpressing tumor cells. Aurora kinase B, a serine/threonine protein kinase that functions in the attachment of the mitotic spindle to the centromere, is overexpressed in a wide variety of cancer cell types.

2-(3-{[7-(3-Chloropropoxy)quinazolin-4-yl]amino}-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide and 2-(ethylamino)ethanol (ideally 12 molar equivalents) were added to N, N-dimethylacetamide under an inert atmosphere (such as provided by nitrogen) and the mixture heated to 90° C. with stirring. 2-(3-{[7-(3-Chloropropoxy)quinazolin-4-yl]amino}-lH-pyrazol-5-yl)-N-(3- fluorophenyl)acetamide and 2-(ethylamino)ethanol (12 molar equivalents) were added to N, N-dimethylacetamide under an inert atmosphere (such as provided by nitrogen) and the mixture heated to 9O2-(3-{[7-(3-Chloropropoxy)quinazolin-4-yl]amino}-lH-pyrazol-5-yl)-N-(3- fluorophenyl)acetamide and 2-(ethylamino)ethanol (ideally 12 molar equivalents) were added to N, N-dimethylacetamide under an inert atmosphere (such as provided by nitrogen) and the mixture heated to 90

AZD1152-HQPA is a a highly selective inhibitor of aurora-B kinase. AZD1152-HQPA has been shown to inhibit osteosarcoma cell line U2-OS cells proliferation. AZD1152-HQPA was also shown to be an effective apoptosis-inducing agent in acute myeloid leukemia cell lines and primary acute myeloid leukemia cultures.

Molecular Weight:507.6
XLogP3:3
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:13
Exact Mass:507.23941601
Monoisotopic Mass:507.23941601
Topological Polar Surface Area:128
Heavy Atom Count:37
Complexity:693
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes