abcr has an exclusive partnership with Bellen for the distribution of catalog compound in Europe. A great opportunity to bundle building blocks, catalysts and reagents in the same order. abcr GmbH is responsible for small quantities of the Bellen productlines Indazole, Quinazoline, Isoquinoline, Quinoline, Pyrozole, Pyridine, Piperidine, Aza-Indazole from gram units up to kg units.
This novel building blocks can be used as hinge binders required for kinase ATP-pocket inhibitors. These hinge binders were designed carefully so that they can form one to three hydrogen bonds to the hinge. They contain one to multiple functional groups at various positions that can be derivatized sequentially.
Kinase inhibitors are a clinically important family of prescription drugs that belong to the class of so called targeted therapy, for the treatment of cancer and more recently in the immunology area for the treatment of arthritis.
Facilitate your SAR studies by switching one of your phenyl group to the bicyclo[1.1.1]pentane. Bicyclo[1.1.1]pentane or 2-F-bicyclo[1.1.1]pentane is a phenyl isostere. It offers the following benefits for this isostere replacement: Maintain the same molecular weight - Increase the sp³ character / reduce
the flatness of the final product - Increase solubility and permeability of the final product - Reduce the clogp and clog D - Increase LELP, LE
(References: J. Med. Chem., 2012, 55, 3414-3424; ChemMedChem 2015, 10, 461-469)
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