5305-59-9Relevant articles and documents
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase
Sisko, John T.,Tucker, Thomas J.,Bilodeau, Mark T.,Buser, Carolyn A.,Ciecko, Patrice A.,Coll, Kathleen E.,Fernandes, Christine,Gibbs, Jackson B.,Koester, Timothy J.,Kohl, Nancy,Lynch, Joseph J.,Mao, Xianzhi,McLoughlin, Debra,Miller-Stein, Cynthia M.,Rodman, Leonard D.,Rickert, Keith W.,Sepp-Lorenzino, Laura,Shipman, Jennifer M.,Thomas, Kenneth A.,Wong, Bradley K.,Hartman, George D.
, p. 1146 - 1150 (2006)
Pyrimidino-thiazolyl carbonitriles were prepared that are potent VEGFR-2 (KDR) kinase inhibitors. The modification of lead structures resulted in 3m which exhibited the best overall profile in KDR inhibitory activity, iv/po pharmacokinetics, and reduced hERG affinity.
Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance
Fischer, Tim,Najjar, Karim,Totzke, Frank,Sch?chtele, Christoph,Sippl, Wolfgang,Ritter, Christoph,Hilgeroth, Andreas
, p. 1 - 8 (2017/11/14)
With ongoing resistance problems against the marketed EGFR inhibitors having a quinazoline core scaffold there is a need for the development of novel inhibitors having a modified scaffold and, thus, expected lower EGFR resistance problems. An additional problem concerning EGFR inhibitor resistance is an observed heterodimerization of EGFR with PDGFR-β that neutralises the sole inhibitor activity towards EGFR. We developed novel pyrimido[4,5-b]indoles with varied substitution patterns at the 4-anilino residue to evaluate their EGFR and PDGFR-β inhibiting properties. We identified dual inhibitors of both EGFR and PDGFR-β in the nanomolar range which have been initially screened in cancer cell lines to prove a benefit of both EGFR and PDGFR-β inhibition.
BTK INHIBITOR
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Paragraph 0346-0347, (2017/11/16)
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).