- A diaryl tetrapyran and pyrimidine derivatives and their medical use
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The invention relates to a dihydropyran pyrimidine derivatives with the structure of formula (I), and (or) pharmaceutically acceptable salts, and pharmaceutical application thereof as Hedgehog signal transduction inhibitors.
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Paragraph 0152; 0163-0167
(2017/12/04)
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- Design, synthesis, and biological study of 6,7-dihydro-5H-pyrano[2,3-d] pyrimidine derivatives as novel hedgehog signaling pathway inhibitors
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A novel series of hedgehog signaling pathway inhibitors were designed by replacing the pyrimidine nucleus of our earlier reported compounds with 6,7-dihydro-5H-pyrano[2,3-d]pyrimidine scaffold. Among this new class of hedgehog signaling pathway inhibitors, compounds 14 and 18 exhibited promising potency in vitro compared to GDC-0449. Compound 18 was advanced to profile its pharmacokinetic characteristics, and showed moderate pharmacokinetic properties in vivo, indicating that the 6,7-dihydro-5H-pyrano[2,3-d]pyrimidine skeleton is a promising scaffold for further exploration as hedgehog signaling pathway inhibitors. Springer Science+Business Media 2014.
- Xin, Minhang,Zhang, Liandi,Shen, Han,Wen, Jun,Tu, Chongxing,Liu, Zhaoyu,Cheng, Lingfei,Zhao, Xinge
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p. 3784 - 3792
(2014/08/05)
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