Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold

doi:10.1016/j.bmc.2011.05.038

Residential College	false
Status	已發表Published
	Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold
	Zhao A.; Gao X.; Wang Y.; Ai J.; Wang Y.; Chen Y.; Geng M.; Zhang A.
	2011-07-01
Source Publication	Bioorganic and Medicinal Chemistry
ISSN	09680896 14643391
Volume	19 Issue:13 Pages:3906-3918
Abstract	A series of thieno[2,3-d]pyrimidines and furo[2,3-d]pyrimidines were synthesized and evaluated for the c-Met inhibition. Thieno[2,3-d]pyrimidine 6b stood out as the most potent showing an IC of 35.7 nM. This compound displayed high inhibitory effect on cell proliferation in BaF3-TPR-Met cells and showed high selectivity for c-Met family against other 14 tested kinases. However, compound 6b was found ineffective in the c-Met-dependent U-87MG human gliobastoma xenograft model that may be relevant to its poor PK profile. © 2011 Elsevier Ltd. All rights reserved.
Keyword	Antitumor C-met Furo[2,3-d]Pyrimidine Rtk Thieno[2,3-d]Pyrimidine
DOI	10.1016/j.bmc.2011.05.038
URL	View the original
Language	英語English
WOS ID	WOS:000291934700004
Scopus ID	2-s2.0-79959518655
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics
Document Type	Journal article
Collection	University of Macau
Affiliation	Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Recommended Citation GB/T 7714	Zhao A.,Gao X.,Wang Y.,et al. Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold[J]. Bioorganic and Medicinal Chemistry, 2011, 19(13), 3906-3918.
APA	Zhao A.., Gao X.., Wang Y.., Ai J.., Wang Y.., Chen Y.., Geng M.., & Zhang A. (2011). Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold. Bioorganic and Medicinal Chemistry, 19(13), 3906-3918.
MLA	Zhao A.,et al."Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold".Bioorganic and Medicinal Chemistry 19.13(2011):3906-3918.

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