24966-31-2Relevant academic research and scientific papers
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase
Newton, Rebecca,Waszkowycz, Bohdan,Seewooruthun, Chitra,Burschowsky, Daniel,Richards, Mark,Hitchin, Samantha,Begum, Habiba,Watson, Amanda,French, Eleanor,Hamilton, Niall,Jones, Stuart,Lin, Li-Ying,Waddell, Ian,Echalier, Aude,Bayliss, Richard,Jordan, Allan M.,Ogilvie, Donald
, p. 497 - 505 (2020)
A combination of focused library and virtual screening, hit expansion, and rational design has resulted in the development of a series of inhibitors of RETV804M kinase, the anticipated drug-resistant mutant of RET kinase. These agents do not inhibit the wild type (wt) isoforms of RET or KDR and therefore offer a potential adjunct to RET inhibitors currently undergoing clinical evaluation.
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors
Frey, Robin R.,Curtin, Michael L.,Albert, Daniel H.,Glaser, Keith B.,Pease, Lori J.,Soni, Niru B.,Bouska, Jennifer J.,Reuter, David,Stewart, Kent D.,Marcotte, Patrick,Bukofzer, Gail,Li, Junling,Davidsen, Steven K.,Michaelides, Michael R.
supporting information; experimental part, p. 3777 - 3787 (2009/04/07)
7-Aminopyrazolo[1,5-a]pyrimidine urea receptor tyrosine kinase inhibitors have been discovered. Investigation of structure-activity relationships of the pyrazolo[1,5-a]pyrimidine nucleus led to a series of 6-(4-N,N′-diphenyl) ureas that potently inhibited
Potential antimalarials. XXII Some 2,4-diamino-5-(3- and 4-trifluoromethylphenyl and 3,4-methylenedioxyphenyl)pyrimidines
Barlin, Gordon B.,Kotecka, Barbara,Rieckmann, Karl H.
, p. 647 - 650 (2007/10/03)
A series of 10 pyrimethamine analogues containing 3′- and 4′-trifluoromethyl and 3′,4′-methylenedioxy groups has been prepared and tested for in vitro antimalarial activity against the FC-27 and K-1 isolates of Plasmodium falciparum. Several of these compounds were almost as active as pyrimethamine against the drug-sensitive FC-27 isolate, and like pyrimethamine, they were much less active against the drug-resistant K-1 isolate. The 4′-trifluoromethyl compunds, however, showed much smaller differences.
