Results 221 to 230 of about 17,593 (256)

Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

Journal of Medicinal Chemistry, 2011
An aryloxy tetramethylcyclobutane was identified as a novel template for androgen receptor (AR) antagonists via cell-based high-throughput screening. Follow-up to the initial "hit" established 5 as a viable lead. Further optimization to achieve full AR antagonism led to the discovery of 26 and 30, both of which demonstrated excellent in vivo tumor ...
Chuangxing, Guo, Angelica, Linton, Susan, Kephart, Martha, Ornelas, Mason, Pairish, Javier, Gonzalez, Samantha, Greasley, Asako, Nagata, Benjamin J, Burke, Martin, Edwards, Natilie, Hosea, Ping, Kang, Wenyue, Hu, Jon, Engebretsen, David, Briere, Manli, Shi, Hovik, Gukasyan, Paul, Richardson, Kevin, Dack, Toby, Underwood, Patrick, Johnson, Andrew, Morell, Robert, Felstead, Hidetoshi, Kuruma, Hiroaki, Matsimoto, Amina, Zoubeidi, Martin, Gleave, Gerrit, Los, Andrea N, Fanjul   +28 more
openaire   +2 more sources

ChemInform Abstract: Recent Developments in Androgen Receptor Antagonists

ChemInform, 2015
AbstractReview: 78 refs.
Fansheng Ran, Hualu Xing, Yang Liu, Daoguang Zhang, Pengzhan Li, Guisen Zhao   +5 more
openaire   +1 more source

A Chemoenzymatic Synthesis of an Androgen Receptor Antagonist

Organic Process Research & Development, 2007
A new scalable enzymatic resolution approach to both enantiomers of trans-2-hydroxycyclohexanecarbonitrile (9 and 11) was developed. Treatment of the racemic mixture (4) with succinic anhydride in the presence of Novozym 435 led to selective acylation of one enantiomer to the corresponding hemisuccinate, which was separated from the unreacted ...
Rajappa Vaidyanathan, Lynsey Hesmondhalgh, Shanghui Hu   +2 more
openaire   +1 more source

Triterpenes from Alisma orientalis act as androgen receptor agonists, progesterone receptor antagonists, and glucocorticoid receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2014
Alisma orientalis, a well-known traditional medicine, exerts numerous pharmacological effects including anti-diabetes, anti-hepatitis, and anti-diuretics but its bioactivity is not fully clear. Androgen receptor (AR), progesterone receptor (PR), and glucocorticoid receptor (GR) are three members of nuclear receptor superfamily that has been widely ...
openaire   +2 more sources

Androgen receptor antagonist suppresses exercise-induced hypertrophy of skeletal muscle

European Journal of Applied Physiology and Occupational Physiology, 1994
The physiological importance of the increase in androgen receptors in exercise-induced muscle hypertrophy was investigated in rats. Together with training rat gastrocnemius muscles by electrical stimulation every other day for 2 weeks, male rats were administered the androgen receptor antagonist, oxendolone. The androgen receptor antagonist effectively
K, Inoue, S, Yamasaki, T, Fushiki, Y, Okada, E, Sugimoto   +4 more
openaire   +2 more sources

Computationally Identified Novel Diphenyl- and Phenylpyridine Androgen Receptor Antagonist Structures

Journal of Chemical Information and Modeling, 2008
We have identified and profiled a set of androgen receptor (AR) binding compounds representing two nonsteroidal scaffolds from a public chemical database supplied by Asinex with virtual screening procedure incorporating our recently published 3D QSAR model of AR ligands.
Annu A, Söderholm, Johanna, Viiliäinen, Pekka T, Lehtovuori, Hanna, Eskelinen, Daniela, Roell, Aria, Baniahmad, Tommi H, Nyrönen   +6 more
openaire   +2 more sources

Discovery of novel spirocyclic derivates as potent androgen receptor antagonists

Bioorganic & Medicinal Chemistry
We report herein the development of a series of novel AR antagonists characterized by a spirocyclic scaffold, employing scaffold hopping and structure-based drug design strategies. Most of the spirocyclic derivatives exhibited enhanced AR antagonistic activity and superior antiproliferative activity against LNCaP cells compared to enzalutamide.
Wenqiang, Zhang, Xiaoyu, Zhou, Hao, Zhu, Yawen, Fan, Zhuolin, Chen, Chenxiao, Wang, Xingru, Chen, Hongmei, Li, Tao, Lu, Xian, Wei, Yadong, Chen, Caiping, Chen, Yu, Jiao   +12 more
openaire   +2 more sources

Systemic therapy for hormone receptor‐positive/human epidermal growth factor receptor 2‐negative early stage and metastatic breast cancer

Ca-A Cancer Journal for Clinicians, 2023
Laura A Huppert, Hope S Rugo
exaly  

Chimeric antigen receptor T‐cell therapy in multiple myeloma: A comprehensive review of current data and implications for clinical practice

Ca-A Cancer Journal for Clinicians, 2023
Rujul Parikh
exaly  

Critical care management of chimeric antigen receptor T‐cell therapy recipients

Ca-A Cancer Journal for Clinicians, 2022
Alexander Shimabukuro-Vornhagen, Victoria Metaxa, Elie Azoulay   +2 more
exaly