Hatcher, John M.; Bahcall, Magda; Choi, Hwan Geun; Gao, Yang; Sim, Taebo; George, Rani; Janne, Pasi A.; Gray, Nathanael S. published their research in Journal of Medicinal Chemistry on December 10 ,2015. The article was titled 《Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation》.COA of Formula: C14H26BN3O2 The article contains the following contents:
The treatment of patients with advanced nonsmall-cell lung cancer harboring chromosomal rearrangements of anaplastic lymphoma kinase (ALK) has been revolutionized by the development of crizotinib, a small-mol. inhibitor of ALK, ROS1, and MET. However, resistance to crizotinib inevitably develops through a variety of mechanisms, leading to relapse both systemically and in the central nervous system (CNS). This has motivated the development of “”second-generation”” ALK inhibitors, including alectinib and ceritinib, that overcome some of the mutations leading to resistance. However, most of the reported ALK inhibitors do not show inhibition of the G1202R mutant, which is one of the most common mutations. Herein, the authors report the development of a structural analog of alectinib I that is potent against the G1202R mutant as well as a variety of other frequently observed mutants. In addition, I is capable of penetrating the CNS of mice following oral dosing. In the experiment, the researchers used N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine(cas: 847818-72-8COA of Formula: C14H26BN3O2)
N,N-Dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole-1-propanamine(cas: 847818-72-8) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. COA of Formula: C14H26BN3O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics