Design, Synthesis, and Biological Evaluation 16-Substituted 4-Azasteroids as Tissue-Selective Androgen Receptor Modulators (SARMs)

被引：13

作者：

Mitchell, Helen J. ^{[1
]}

Dankulich, William P. ^{[1
]}

Hartman, George D. ^{[1
]}

Prueksaritanont, Thomayant ^{[3
]}

Schmidt, Azriel ^{[2
]}

Vogel, Robert L. ^{[2
]}

Bai, Chang ^{[2
]}

McElwee-Witmer, Sheila ^{[2
]}

Zhang, Hai Z. ^{[2
]}

Chen, Fang ^{[2
]}

Leu, Chih-Tai ^{[2
]}

Kimmel, Donald B. ^{[2
]}

Ray, William J. ^{[2
]}

Nantermet, Pascale ^{[2
]}

Gentile, Michael A. ^{[2
]}

Duggan, Mark E. ^{[1
]}

Meissner, Robert S. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

[2] Merck Res Labs, Dept Mol Endocrinol, West Point, PA 19486 USA

[3] Merck Res Labs, Dept Drug Metab, West Point, PA 19486 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 15期

关键词：

REPLACEMENT THERAPY; AGING MALE; TESTOSTERONE;

D O I：

10.1021/jm900880r

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 16-substiuted-4-azasteroids has been identified as potential tissue-selective androgen receptor modulators. These ligands display potent hAR binding and agonist activity, low virilizing potential,and good pharmacokinetic profiles in dogs. On the basis of its in vitro profile, 21 was evaluated in the OVX and ORX rat models and exhibited all osteoanabolic, tissue-selective profile.

引用

页码：4578 / 4581

页数：4

共 50 条

[21] Design and synthesis of an array of selective androgen receptor modulators
Trump, Ryan P.
Blanc, Jean-Baptiste E.
Stewart, Eugene L.
Brown, Peter J.
Caivano, Matilde
Gray, David W.
Hoekstra, William J.
Willson, Timothy M.
Han, Bajin
Turnbull, Philip
JOURNAL OF COMBINATORIAL CHEMISTRY, 2007, 9 (01): : 107 - 114
[22] Design and synthesis of an array of selective androgen receptor modulators
Trump, RP
Turnbull, P
Blanc, JBE
Wiethe, RW
Stewart, EL
Caivano, M
Gray, D
Hoekstra, WJ
Willson, TM
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2508 - U2508
[23] Tissue Selective Androgen Receptor Modulators (SARMs) Increase Pelvic Floor Muscle Mass in Ovariectomized Mice
Ponnusamy, Suriyan
Sullivan, Ryan D.
Thiyagarajan, Thirumagal
Tillmann, Heather
Getzenberg, Robert H.
Narayanan, Ramesh
JOURNAL OF CELLULAR BIOCHEMISTRY, 2017, 118 (03) : 640 - 646
[24] Synthesis of isothiocyanate derivatives of irreversible selective androgen receptor modulators (SARMs) and biological testing in prostate cancer cell lines.
Hwang, DJ
Chen, JY
Xu, HP
Mustafa, SM
Dalton, JT
Miller, DD
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U140 - U140
[25] Design, synthesis, and biological evaluation of nonssteroidal selective glucocorticoid receptor modulators
McMaster, Danielle M.
Mitchell, Helen J.
Schmidt, Azriel
Hershey, James C.
Bai, Chang
Brandish, Philip E.
Vogel, Robert L.
Leu, Chi-Tai
Gambone, Carlo
McElwee-Witmer, Sheila
Meissner, Robert S.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 238
[26] Design, synthesis and biological evaluation of ortho-substituted phenethyl pyrazoles as selective glucocorticoid receptor modulators (SEGRMs)
Perkins, James J.
Bungard, Christopher
Brandish, Philip
Darimont, Beatrice
Euler, Danielle
Gambone, Carlo
Hershey, James
Leu, Chih-Tai
Manikowski, Jesse J.
McElwee-Witmer, Sheila
McIntosh, Ian
Schmidt, Azriel
Thompson, Charles
Vogel, Robert
Meissner, Robert
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2010, 239
[27] Synthesis and androgen receptor affinity of several linkages of 1,3-disubstituted-2-hydroxy-2-methylpropionamide selective androgen receptor modulators (SARMs).
Hwang, DJ
Kim, J
Dalton, JT
Miller, DD
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U139 - U139
[28] Design, Synthesis, and Biological Evaluation of Nonsteroidal Cycloalkane[d]isoxazole-Containing Androgen Receptor Modulators
Poutiainen, Pekka K.
Oravilahti, Tuomas
Perakyla, Mikael
Palvimo, Jorma J.
Ihalainen, Janne A.
Laatikainen, Reino
Pulkkinen, Juha T.
JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (14) : 6316 - 6327
[29] Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators
Singla, Ramit
Gupta, Kunj Bihari
Upadhyay, Shishir
Dhiman, Monisha
Jaitak, Vikas
BIOORGANIC & MEDICINAL CHEMISTRY, 2018, 26 (01) : 266 - 277
[30] Design, Synthesis, Biological Evaluation and SARs of Novel N-Substituted Sulfoximines as Potential Ryanodine Receptor Modulators
Xie, Yongtao
Zhou, Sha
Li, Yuxin
Zhou, Shaa
Chen, Minggui
Wang, Baolei
Xiong, Lixia
Yang, Na
Li, Zhengming
CHINESE JOURNAL OF CHEMISTRY, 2018, 36 (02) : 129 - 133

← 1 2 3 4 5 →