651305-84-9Relevant academic research and scientific papers
Discovery of novel isothiazole inhibitors of the TrkA kinase: Structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists
Lippa, Blaise,Morris, Joel,Corbett, Matthew,Kwan, Tricia A.,Noe, Mark C.,Snow, Sheri L.,Gant, Thomas G.,Mangiaracina, Melchiorra,Coffey, Heather A.,Foster, Barbara,Knauth, Elisabeth A.,Wessel, Matthew D.
, p. 3444 - 3448 (2007/10/03)
The design, synthesis, and biological evaluation of potent inhibitors of the TrkA kinase is presented. A homology model is created to aid in the enhancement of potency and selectivity of isothiazole inhibitors found during a high-throughput screen. Three different syntheses are utilized to make diverse analogs within this series. Aminoheterocycles are found to be good urea surrogates, whereas bicyclic substituents on the C3 thio group were found to be extremely potent TrkA inhibitors in kinase and cell assays.
ISOTHIAZOLE DERIVATIVES USEFUL AS ANTICANCER AGENTS
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Page 33, (2010/02/06)
The invention relates to compounds of the formula 1 or pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof, wherein X, R1, and R2 are as defined herein. The invention also relates to pharmaceutical compositions
