Jansa, Josef published the artcileImidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid, the publication is European Journal of Medicinal Chemistry (2021), 113309, database is CAplus and MEDLINE.
Pharmacol. inhibition of cyclin-dependent kinases has emerged as a possible treatment option for various cancer types. Authors recently identified substituted imidazo[1,2-c]pyrimidin-5(6H)-ones as inhibitors of cyclin-dependent kinase 2 (CDK2). Here, the synthesis of derivatives modified at positions 2, 3, 6 or 8 prepared using Suzuki-Miyaura cross-coupling, halogenation, Dimroth-type rearrangement and alkylation as the main synthetic methods was reported. The compounds displayed micro- to submicromolar inhibition of CDK2/cyclin E activity. Binding of the most potent compound I to CDK2 was determined using isothermal titration calorimetry. The co-crystal structure of I in complex with fully active CDK2 was solved, revealing the binding mode of I in the ATP pocket and a hydrogen bonding interaction with hinge region residue Leu83. Evaluation against leukemia cell lines revealed low cytotoxicity, which is in line with the high selectivity towards CDK2. This study demonstrates that substituted imidazo[1,2-c]pyrimidines can be exploited for future kinase inhibitor development.
European Journal of Medicinal Chemistry published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Recommanded Product: 2-Chloro-4-hydroxyphenylboronic acid.
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