252003-31-9Relevant 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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, (2008/06/13)
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2and R3are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
