Design, synthesis, and evaluation of pyrrolo [2, 1-f][1, 2, 4] triazine derivatives as novel hedgehog signaling pathway inhibitors

…, F Tang, C Tu, J Wen, X Zhao, Z Liu, L Cheng…

Index: Xin, Minhang; Zhang, Liandi; Tang, Feng; Tu, Chongxing; Wen, Jun; Zhao, Xinge; Liu, Zhaoyu; Cheng, Lingfei; Shen, Han Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 4 p. 1429 - 1440

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Citation Number: 17

Abstract

Abstract 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 ...