- Heterocyclic amines Hedgehog signal pathway inhibitor
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The invention relates to the field of biological medicine, in particular to a heterocyclic amine compound and an application thereof, namely a general formula (I) compound and acceptable salt in the pharmaceutical field. The compound can be used in the Hedgehog signal transduction inhibitor application and various medical applications (please see the formula in the specification). The invention further relates to a preparation method with the general formula (I).
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Paragraph 0154-0155; 0160-0161; 0240; 0247-0248; 0341; 0352
(2017/10/06)
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- Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors
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A novel series of Hh signaling pathway inhibitors were designed by replacing the pyrimidine skeleton of our earlier reported lead compound 1 with pyrrolo[2,1-f][1,2,4]triazine scaffold. Starting from this new scaffold, SAR exploration was investigated based on structural modification on A-ring, C-ring and D-ring. And several much potent compounds were studies in vivo to profile their pharmacokinetic properties. Finally, optimization leads to the identification of compound 19a, a potent Hh signaling pathway inhibitor with superior potency in vitro and satisfactory pharmacokinetic properties in vivo.
- Xin, Minhang,Zhang, Liandi,Tang, Feng,Tu, Chongxing,Wen, Jun,Zhao, Xinge,Liu, Zhaoyu,Cheng, Lingfei,Shen, Han
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p. 1429 - 1440
(2014/03/21)
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