Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors.

Shinya Nagashima,Hiroshi Nagata,Masahiro Iwata,Masaki Yokota,Hiroyuki Moritomo,Masaya Orita,Sadao Kuromitsu,Akiko Koakutsu,Keiko Ohga,Makoto Takeuchi,Mitsuaki Ohta,Shin-ichi Tsukamoto

Bioorganic & Medicinal Chemistry（2008）

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摘要

The novel 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivative 25y (YM-341619, AS1617612) potently inhibited STAT6 activation and Th2 differentiation with IC50 values of 0.70 and 0.28nM, respectively, and showed an oral bioavailability of 25% in mouse.

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关键词

Signal transducers and activators of transcription 6,Allergic disease,Interleukin-4,Th2 differentiation

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