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

[1] MEDI 319-Design, synthesis and biological evaluation of 16-substituted-4-azasteroids as tissue-selective androgen receptor modulators
Mitchell, Helen J.
Dankulich, William P.
Bai, Chang
Prueksaritanont, Thomayant
Schmidt, Azriel
Chen, Fang
Kimmel, Donald B.
Meissner, Robert S.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2008, 236
[2] MEDI 165-Design, synthesis, and biological evaluation of 17-thiazole-4-azasteroids as tissue-selective androgen receptor modulators
Kaufman, Mildred L.
Mitche, Helen J.
Hartman, George D.
Prueksaritanont, Thomayant
Schmidt, Azriel
Bai, Chang
Chen, Fang
Kimmel, Donald B.
Duggan, Mark E.
Meissner, Robert S.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 234
[3] MEDI 317-Design, synthesis and biological evaluation of 6-substituted-4-azasteroids as tissue selective androgen receptor modulators
McVean, Carol A.
Wang, Jiabing
Bai, Chang
Chen, Fang
Kimmel, Donald B.
Prueksaritanont, Thomayant
Schmidt, Azriel
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2008, 236
[4] MEDI 271-Design, synthesis and biological evaluation of Benzamide Derivatives as tissue-selective androgen receptor modulators
Hanney, Barbara A.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2008, 235
[5] Tissue-Selective Androgen Receptor Modulators (SARMs) for the treatment of Duchenne muscular dystrophy (DMD)
Ponnusamy, S.
Sullivan, R.
Zafar, N.
Narayanan, R.
NEUROMUSCULAR DISORDERS, 2016, 26 : S130 - S130
[6] Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I
Aikawa, Katsuji
Miyawaki, Toshio
Hitaka, Takenori
Imai, Yumi N.
Hara, Takahito
Miyazaki, Junichi
Yamaoka, Masuo
Kusaka, Masami
Kanzaki, Naoyuki
Tasaka, Akihiro
Shiraishi, Mitsuru
Yamamoto, Satoshi
BIOORGANIC & MEDICINAL CHEMISTRY, 2015, 23 (10) : 2568 - 2578
[7] Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs)
Miller, Chris P.
Bhaket, Pushpal
Muthukaman, Nagarajan
Lyttle, C. Richard
Shomali, Maysoun
Gallacher, Kyla
Slocum, Connie
Hattersley, Gary
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (24) : 7516 - 7520
[8] Androgen therapy using tissue-selective androgen receptor modulators
Negro-Vilar, A.
INTERNATIONAL JOURNAL OF ANDROLOGY, 2005, 28 : 18 - 18
[9] Development of new tissue-selective androgen receptor modulators
Grootenhuis, A. J.
INTERNATIONAL JOURNAL OF ANDROLOGY, 2005, 28 : 19 - 19
[10] Selective androgen receptor modulators: In pursuit of tissue-selective androgens
Omwancha, Josephat
Brown, Terry R.
CURRENT OPINION IN INVESTIGATIONAL DRUGS, 2006, 7 (10) : 873 - 881

← 1 2 3 4 5 →