Zobrazeno 1 - 10
of 11
pro vyhledávání: '"James J. Fiordeliso"'
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
Publikováno v:
Journal of Heterocyclic Chemistry. 43:1391-1396
When a known 2-[4-morpholino]-3-aryl-5-substituted thiophene, which showed moderate activity as a progesterone antagonist, was superimposed with a potent steroidal progesterone antagonist Org-33628, it showed a fair alignment in most parts of the mol
Autor:
Zhihua Sui, Vernon C. Alford, Olivia Linton, Xuqing Zhang, Ronald K. Russell, George F. Allan, Muh-Tsann Lai, James C. Lanter, Scott G. Lundeen, Kenneth M. Wells, James J. Fiordeliso
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(9)
Through an in vivo screening model, we developed the in vivo SAR of beta-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models an
Autor:
Joseph W. Gunnet, Pamela Tannenbaum, Weiqin Jiang, Scott G. Lundeen, Olivia Linton, Peifang Zhu, Zhihua Sui, Jun Xu, James J. Fiordeliso, George F. Allan, Keith T. Demarest
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(5)
Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-diabetic activities. For glucocorticoid receptor (GR) program, we sought an unexplored, synthetically accessible phosphorus-containing steroidal mim
Autor:
Weiqin Jiang, George F. Allan, Joseph W. Gunnet, Zhihua Sui, James J. Fiordeliso, Xin Chen, Jun Xu, Pamela Tannenbaum, Scott G. Lundeen, Keith T. Demarest, Peifang Zhu, Olivia Linton
Publikováno v:
Steroids. 71(11-12)
A novel series of steroidal compounds were designed and synthesized with various phosphorus-containing groups on the 17β-side chain as progesterone receptor antagonists. The structure-activity relationships of these compounds are discussed. Selected
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(21)
Two potential bioisosteres of the nonsteroidal antiandrogen bicalutamide, an imidazolidinone and an indole, were synthesized and tested for their androgen receptor binding. Indole was discovered to be a suitable bioisostere for the acyl anilide moiet
Autor:
Sheela Bhattacharjee, Donna Haynes-Johnson, Zhihua Sui, Scott G. Lundeen, Olivia Linton, Muh-Tsann Lai, Tifanie Sbriscia, George F. Allan, James C. Lanter, Robert Dodds, James J. Fiordeliso
Publikováno v:
The Journal of steroid biochemistry and molecular biology. 103(1)
The pharmacological activity of JNJ-26146900 is described. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand with tissue-selective activity in rats. The compound was evaluated in in vitro and in vivo models of AR activity. It binds to the
Autor:
Zhihua Sui, Sheela Bhattacharjee, Joanna Clancy, James C. Lanter, James J. Fiordeliso, Elizabeth Craig, Patricia Kraft, T. Mathew John, Weiqin Jiang, Donna Haynes-Johnson, Mark J. Macielag, Yuhong Qiu
Publikováno v:
Journal of medicinal chemistry. 47(3)
The discovery of the potent and selective PDE-5 inhibitory activity of a pyrroloquinolone scaffold prompted us to explore the SAR of its acyl derivatives. During the course of these studies, three structural series were found with K(i) values for PDE
Autor:
Shawn Walsh, Sheela Bhattacharjee, Weiqin Jiang, Mark J. Macielag, Joanna Clancy, Elizabeth Craig, Donna Haynes-Johnson, James C. Lanter, Patricia Kraft, Jihua Guan, Zhihua Sui, T. Matthew John, James J. Fiordeliso, Yuhong Qiu
Publikováno v:
Journal of medicinal chemistry. 46(3)
Synthesis of furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors was reported. Their in vitro potencies in inhibiting PDE5 and selectivity in inhibiting other PDE isozymes (PDE1-4 and PDE6) were evaluated. Some of these c