Formula: C7H15NOIn 2016 ,《Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase》 appeared in Journal of Medicinal Chemistry. The author of the article were Fraser, Craig; Dawson, John C.; Dowling, Reece; Houston, Douglas R.; Weiss, Jason T.; Munro, Alison F.; Muir, Morwenna; Harrington, Lea; Webster, Scott P.; Frame, Margaret C.; Brunton, Valerie G.; Patton, E. Elizabeth; Carragher, Neil O.; Unciti-Broceta, Asier. The article conveys some information:
Novel pyrazolopyrimidines displaying high potency and selectivity toward SRC family kinases have been developed by combining ligand-based design and phenotypic screening in an iterative manner. Compounds were derived from the promiscuous kinase inhibitor PP1 to search for analogs that could potentially target a broad spectrum of kinases involved in cancer. Phenotypic screening against MCF7 mammary adenocarcinoma cells generated target-agnostic structure-activity relationships that biased subsequent designs toward breast cancer treatment rather than to a particular target. This strategy led to the discovery of two potent antiproliferative leads with phenotypically distinct anticancer mode of actions. Kinase profiling and further optimization resulted in eCF506, the first small mol. with subnanomolar IC50 for SRC that requires 3 orders of magnitude greater concentration to inhibit ABL. eCF506 exhibits excellent water solubility, an optimal DMPK profile and oral bioavailability, halts SRC-associated neuromast migration in zebrafish embryos without inducing life-threatening heart defects, and inhibits SRC phosphorylation in tumor xenografts in mice. In the experimental materials used by the author, we found 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Formula: C7H15NO)
2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKFormula: C7H15NO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem