Novel and orally active 5-(1,3,4-oxadiazol-2-yl)pyrimidine derivatives as selective FLT3 inhibitors

The synthesis and structure–activity relationship studies of a novel series of FLT3 inhibitors are described. Compound 23r possesses best efficacy against tumor xenograft model by oral administration. 5-(1,3,4-Oxadiazol-2-yl)pyrimidine derivative 1 was identified as a new class of FLT3 inhibitor fro...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-10, Vol.18 (20), p.5472-5477
Hauptverfasser:	Ishida, Hiroshi, Isami, Shoichi, Matsumura, Tsutomu, Umehara, Hiroshi, Yamashita, Yoshinori, Kajita, Jiro, Fuse, Eiichi, Kiyoi, Hitoshi, Naoe, Tomoki, Akinaga, Shiro, Shiotsu, Yukimasa, Arai, Hitoshi
Format:	Artikel
Sprache:	eng
Schlagworte:	5-(1,3,4-Oxadiazol-2-yl)pyrimidine Administration, Oral Animals Antineoplastic agents Biological and medical sciences Cell Line, Tumor Cell Proliferation Chemistry, Pharmaceutical - methods Drug Design FLT3 inhibitor fms-Like Tyrosine Kinase 3 - antagonists & inhibitors fms-Like Tyrosine Kinase 3 - chemistry General aspects Humans Inhibitory Concentration 50 Medical sciences Mice Mice, SCID Models, Chemical Neoplasm Transplantation Oxadiazoles - chemical synthesis Oxadiazoles - pharmacology Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Structure-Activity Relationship
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