Zobrazeno 1 - 10
of 41
pro vyhledávání: '"George F. Allan"'
Autor:
Nareshkumar F. Jain, Xin Chen, Pamela Tannenbaum, Zhihua Sui, Fu-An Kang, Scott G. Lundeen, George F. Allan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3687-3690
Replacement of the 7-CH2 group of natural steroid with an oxygen atom led to identification of unnatural 7-oxa-steroids as potent and selective progesterone receptor antagonists. The unnatural 7-oxa-steroids exhibited a different structure–activity
Autor:
Zhihua Sui, Raymond A. Ng, Muh-Tsann Lai, Olivia Linton, Scott G. Lundeen, Sheela Bhattacharjee, George F. Allan, Tifanie Sbriscia, Donna Haynes-Johnson
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 110:207-213
Androgens are required for the maintenance of normal sexual activity in adulthood and for enhancing muscle growth and lean body mass in adolescents and adults. Androgen receptor (AR) ligands with tissue selectivity (selective androgen receptor modula
Autor:
Margaret Kiddoe, Olivia Linton, C. Edgar Cook, John A. Kepler, Zhihua Sui, Sheela Bhattacharjee, George F. Allan, Scott G. Lundeen, Chunyang Jin, Govindarajan Manikumar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5754-5757
A series of novel 11β-aryl-4′,5′-dihydrospiro[estra-4,9-diene-17β,4′-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based alkaline phosphatase assay and the A549 cell-based functional assay.
Autor:
Olivia Linton, Tifanie Sbriscia, Xuqing Zhang, George F. Allan, Muh-Tsann Lai, Sheela Bhattacharjee, Zhihua Sui, Donna Haynes-Johnson, Scott G. Lundeen, Pamela Tannenbaum
Publikováno v:
Endocrine. 32:41-51
Androgen receptor (AR) ligands with tissue selectivity (selective androgen receptor modulators, or SARMs) have potential for treating muscle wasting, hypogonadism of aging, osteoporosis, female sexual dysfunction, and other indications. JNJ-28330835
Autor:
Scott G. Lundeen, George F. Allan, Olivia Linton, Xuqing Zhang, Xiaojie Li, Tifanie Sbriscia, Zhihua Sui
Publikováno v:
Journal of Medicinal Chemistry. 50:3857-3869
A novel series of pyrazolines 2 have been designed, synthesized, and evaluated by in vivo screening as tissue-selective androgen receptor modulators (SARMs). Structure-activity relationships (SAR) were investigated at the R1 to R6 positions as well a
Autor:
James C. Lanter, Vernon C. Alford, Tifanie Sbriscia, George F. Allan, Zhihua Sui, Ng Raymond A, Scott G. Lundeen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1784-1787
The synthesis and in vivo SAR of 2-(2,2,2)-trifluoroethyl-benzimidazoles are described. Prostate antagonism and/or levator ani agonism can be modulated by varying the substitution at the 2-position of 5,6-dichloro-benzimidazoles. Potent androgen agon
Autor:
Zhihua Sui, George F. Allan, James C. Lanter, Olivia Linton, Raymond A. Ng, Tifanie Sbriscia, Scott G. Lundeen, Vernon C. Alford, Jihua Guan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:784-788
The synthesis and in vivo SAR of 5,6-dichloro-benzimidazole derivatives as novel selective androgen receptor antagonists are described. During screening of 2-alkyl benzimidazoles, it was found that a trifluoromethyl group greatly enhances antagonist
Autor:
George F. Allan, Peifang Zhu, Joseph W. Gunnet, Olivia Linton, Nareshkumar F. Jain, Keith T. Demarest, Scott G. Lundeen, Jihua Guan, Pamela Tannenbaum, Xin Chen, Fu-An Kang, Jun Xu, Zhihua Sui
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:907-910
A novel series of oxa-steroids 6 derived from (8S, 13S, 14R)-7-oxa-estra-4,9-diene-3,17-dione 1 have been synthesized and identified as potent and selective progesterone receptor antagonists. These novel oxa-steroids showed similar potency to mifepri
Autor:
Muh-Tsann Lai, Weiqin Jiang, Zhihua Sui, James C. Lanter, Do Won Hahn, George F. Allan, Olivia Linton, James J. Fiordeliso, Scott G. Lundeen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:123-126
A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate weight increases in immature rats. Through the use of this paradigm, we were able to identify co
Autor:
James J. Fiordeliso, Scott G. Lundeen, Jun Xu, Joseph W. Gunnet, Keith T. Demarest, Zhihua Sui, George F. Allan, Peifang Zhu, Olivia Linton, Pamela Tannenbaum, Weiqin Jiang
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:6726-6732
A new series of phosphorus-containing 11beta-aryl-substituted steroids have been synthesized in an eight-step sequence involving a palladium-catalyzed coupling reaction to introduce a phosphorus group onto the aromatic ring. The compounds were evalua