1204975-13-2Relevant academic research and scientific papers
Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened
Peukert, Stefan,He, Feng,Dai, Miao,Zhang, Rui,Sun, Yingchuan,Miller-Moslin, Karen,Mcewan, Michael,Lagu, Bharat,Wang, Kate,Yusuff, Naeem,Bourret, Aaron,Ramamurthy, Arun,Maniara, Wieslawa,Amaral, Adam,Vattay, Anthony,Wang, Anlai,Guo, Ribo,Yuan, Jing,Green, John,Williams, Juliet,Buonamici, Silvia,Kelleher, Joseph F.,Dorsch, Marion
, p. 1261 - 1265 (2013/08/23)
First disclosure: Continued optimization provided a novel type of Smoothened (Smo) antagonist based on a pyridazine core. The compound, NVP-LEQ506, currently in phaseI clinical trials, combines high intrinsic potency and good pharmacokinetic properties resulting in excellent efficacy in rodent tumor models of medulloblastoma. Activity against a Smo mutant conferring resistance observed in a previous clinical trial with a competitor compound suggests additional therapeutic potential.
