137129-98-7Relevant academic research and scientific papers
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): Structure-activity relationships leading to the identification of 6-((5 S,9 R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7- triazaspiro[4.4]nonan-7-yl)nico
Watterson, Scott H.,Xiao, Zili,Dodd, Dharmpal S.,Tortolani, David R.,Vaccaro, Wayne,Potin, Dominique,Launay, Michele,Stetsko, Dawn K.,Skala, Stacey,Davis, Patric M.,Lee, Deborah,Yang, Xiaoxia,McIntyre, Kim W.,Balimane, Praveen,Patel, Karishma,Yang, Zheng,Marathe, Punit,Kadiyala, Pathanjali,Tebben, Andrew J.,Sheriff, Steven,Chang, Chiehying Y.,Ziemba, Theresa,Zhang, Huiping,Chen, Bang-Chi,Delmonte, Albert J.,Aranibar, Nelly,McKinnon, Murray,Barrish, Joel C.,Suchard, Suzanne J.,Murali Dhar
experimental part, p. 3814 - 3830 (2010/07/05)
Leukocyte function-associated antigen-1 (LFA-1), also known as CD11a/CD18 or αLβ2, belongs to the β2 integrin subfamily and is constitutively expressed on all leukocytes. The major ligands of LFA-1 include three intercellu
Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway
Castanedo, Georgette M.,Wang, Shumei,Robarge, Kirk D.,Blackwood, Elizabeth,Burdick, Daniel,Chang, Christine,Dijkgraaf, Gerrit J.P.,Gould, Stephen,Gunzner, Janet,Guichert, Oivin,Halladay, Jason,Khojasteh, Cyrus,Lee, Leslie,Marsters Jr., James C.,Murray, Lesley,Peterson, David,Plise, Emile,Salphati, Laurent,De Sauvage, Frederic J.,Wong, Susan,Sutherlin, Daniel P.
scheme or table, p. 6748 - 6753 (2011/01/12)
Potent and efficacious inhibitors of the hedgehog pathway for the treatment of cancer have been prepared using the 2-pyridyl biphenyl amide scaffold common to the clinical lead GDC-0449. Analogs with polar groups in the para-position of the aryl amide ring optimized potency, had minimal CYP inhibition, and possessed good exposure in rats. Compounds 9d and 14f potently inhibited hedgehog signaling as measured by Gli1 mRNA and were found to be equivalent or more potent than GDC-0449, respectively, when studied in a Ptch+/- medulloblastoma allograft model, that is, highly dependent on hedgehog signaling.
