Name: 3-Bromo-4-chloronitrobenzene. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 3-Bromo-4-chloronitrobenzene, is researched, Molecular C6H3BrClNO2, CAS is 16588-26-4, about GDC-0449-A potent inhibitor of the hedgehog pathway. Author is Robarge, Kirk D.; Brunton, Shirley A.; Castanedo, Georgette M.; Cui, Yong; Dina, Michael S.; Goldsmith, Richard; Gould, Stephen E.; Guichert, Oivin; Gunzner, Janet L.; Halladay, Jason; Jia, Wei; Khojasteh, Cyrus; Koehler, Michael F. T.; Kotkow, Karen; La, Hank; La Londe, Rebecca L.; Lau, Kevin; Lee, Leslie; Marshall, Derek; Marsters, James C.; Murray, Lesley J.; Qian, Changgeng; Rubin, Lee L.; Salphati, Laurent; Stanley, Mark S.; Stibbard, John H. A.; Sutherlin, Daniel P.; Ubhayaker, Savita; Wang, Shumei; Wong, Susan; Xie, Minli.
SAR for a wide variety of heterocyclic replacements for a benzimidazole led to the discovery of functionalized 2-pyridyl amides as novel inhibitors of the hedgehog pathway. The 2-pyridyl amides were optimized for potency, PK, and drug-like properties by modifications to the amide portion of the mol. resulting in I (GDC-0449). Amide I produced complete tumor regression at doses as low as 12.5 mg/kg BID in a medulloblastoma allograft mouse model that is wholly dependent on the Hh pathway for growth and is currently in human clin. trials, where it is initially being evaluated for the treatment of BCC.
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