871024-38-3Relevant articles and documents
PYRROPYRIMIDINE COMPOUNDS AS MNKS INHIBITORS
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Page/Page column 35; 36, (2017/06/12)
The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO-NR8R9, wherein R8 and R9 are each independently
Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d] pyrimidine derivatives: Novel VEGFR2 kinase inhibitors binding to inactive kinase conformation
Oguro, Yuya,Miyamoto, Naoki,Okada, Kengo,Takagi, Terufumi,Iwata, Hidehisa,Awazu, Yoshiko,Miki, Hiroshi,Hori, Akira,Kamiyama, Keiji,Imamura, Shinichi
experimental part, p. 7260 - 7273 (2010/11/18)
We synthesized a series of pyrrolo[3,2-d]pyrimidine derivatives and evaluated their application as type-II inhibitors of vascular endothelial growth factor receptor 2 (VEGFR2) kinase. Incorporation of a diphenylurea moiety at the C4-position of the pyrrolo[3,2-d]pyrimidine core via an oxygen linker resulted in compounds that were potent inhibitors of VEGFR2 kinase. Of these derivatives, compound 20d showed the strongest inhibition of VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC). The co-crystal structure of 20d and VEGFR2 revealed that 20d binds to the inactive form of VEGFR2. Further studies indicated that 20d inhibited VEGFR2 kinase with slow dissociation kinetics and also inhibited PDGFR and Tie-2 kinases. Oral administration of the hydrochloride salt of 20d at 3 mg/kg/day showed potent inhibition of tumor growth in a DU145 human prostate cancer cell xenograft nude mouse model.
FUSED HETEROCYCLIC COMPOUND
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Page/Page column 45, (2009/10/01)
The present invention provides a fused heterocyclic compound having a tyrosine kinase inhibitory action, which is represented by the formula: wherein R1 is a hydrogen atom, a halogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom; R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to each other to form an optionally substituted ring structure; R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to the carbon atom on ring A to form an optionally substituted ring structure; ring A is an optionally substituted benzene ring; and ring B is (i) an optionally substituted fused ring, or (ii) a pyridine ring having optionally substituted carbamoyl (the pyridine ring is optionally further substituted).