118665-02-4Relevant articles and documents
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist
Scott, James S.,Moss, Thomas A.,Balazs, Amber,Barlaam, Bernard,Breed, Jason,Carbajo, Rodrigo J.,Chiarparin, Elisabetta,Davey, Paul R. J.,Delpuech, Oona,Fawell, Stephen,Fisher, David I.,Gagrica, Sladjana,Gangl, Eric T.,Grebe, Tyler,Greenwood, Ryan D.,Hande, Sudhir,Hatoum-Mokdad, Holia,Herlihy, Kara,Hughes, Samantha,Hunt, Thomas A.,Huynh, Hoan,Janbon, Sophie L. M.,Johnson, Tony,Kavanagh, Stefan,Klinowska, Teresa,Lawson, Mandy,Lister, Andrew S.,Marden, Stacey,McGinnity, Dermot F.,Morrow, Christopher J.,Nissink, J. Willem M.,O'Donovan, Daniel H.,Peng, Bo,Polanski, Radoslaw,Stead, Darren S.,Stokes, Stephen,Thakur, Kumar,Throner, Scott R.,Tucker, Michael J.,Varnes, Jeffrey,Wang, Haixia,Wilson, David M.,Wu, Dedong,Wu, Ye,Yang, Bin,Yang, Wenzhan
supporting information, p. 14530 - 14559 (2021/01/05)
Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER+breast cancer. Structure based design together with systematic investigation of each region of the molecular architecture led to the identification of N-[1-(3-fluoropropyl)azetidin-3-yl]-6-[(6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl]pyridin-3-amine (28). This compound was demonstrated to be a highly potent SERD that showed a pharmacological profile comparable to fulvestrant in its ability to degrade ERα in both MCF-7 and CAMA-1 cell lines. A stringent control of lipophilicity ensured that 28 had favorable physicochemical and preclinical pharmacokinetic properties for oral administration. This, combined with demonstration of potent in vivo activity in mouse xenograft models, resulted in progression of this compound, also known as AZD9833, into clinical trials.
Pd-tBuONO Cocatalyzed Aerobic Indole Synthesis
Ning, Xiao-Shan,Liang, Xin,Hu, Kang-Fei,Yao, Chuan-Zhi,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 1590 - 1594 (2018/04/30)
A Pd-tBuONO co-catalyzed scalable and practical synthesis of indoles with molecular oxygen as terminal oxidant is developed. Either terminal or internal 2-vinylanilines could be smoothly converted to desired indoles under one general condition. This method has been evaluated in the large scale synthesis of indomethacin and a potential anti-breast cancer drug candidate 1. (Figure presented.).
A new method for the synthesis of 2,6-dinitro and 2-halo-6-nitrostyrenes
Mundla
, p. 6319 - 6321 (2007/10/03)
A new method for the synthesis of 2-halo-6-nitrostyrenes from 2-halo-6-nitrotoluenes is disclosed. Also described is a one-pot process for the synthesis of 2,6-dinitristyrene from 2,6-dinitrotoluene. (C) 2000 Elsevier Science Ltd.