Search Results - "UNWALLA, R. J"

Optimization of 3-(1H-Indazol-3-ylmethyl)-1,5-benzodiazepines as Potent, Orally Active CCK-A Agonists by Henke, Brad R, Aquino, Christopher J, Birkemo, Larry S, Croom, Dallas K, Dougherty, Robert W, Ervin, Gregory N, Grizzle, Mary K, Hirst, Gavin C, James, Michael K, Johnson, Michael F, Queen, Kennedy L, Sherrill, Ronald G, Sugg, Elizabeth E, Suh, Edward M, Szewczyk, Jerzy W, Unwalla, Rayomand J, Yingling, Jeff, Willson, Timothy M

“…We previously described a series of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepine CCK-A agonists exemplified by compound 1 (GW 5823), which is the first…”
Get full text

3-[2-(N-Phenylacetamide)]-1,5-benzodiazepines:  Orally Active, Binding Selective CCK-A Agonists by Willson, Timothy M, Henke, Brad R, Momtahen, Tanya M, Myers, Peter L, Sugg, Elizabeth E, Unwalla, Rayomand J, Croom, Dallas K, Dougherty, Robert W, Grizzle, Mary K, Johnson, Michael F, Queen, Kennedy L, Rimele, Thomas J, Yingling, Jeffrey D, James, Michael K

“…A series of modifications were made to the C-3 substituent of the 1,5-benzodiazepine CCK-A agonist 1. Replacement of the inner urea NH and addition of a methyl…”
Get full text

Design, Synthesis, and Preclinical Characterization of Novel, Highly Selective Indole Estrogens by Miller, Chris P, Collini, Michael D, Tran, Bach D, Harris, Heather A, Kharode, Yogendra P, Marzolf, James T, Moran, Robert A, Henderson, Ruth A, Bender, Reinhold H. W, Unwalla, Rayomond J, Greenberger, Lee M, Yardley, John P, Abou-Gharbia, Magid A, Lyttle, C. Richard, Komm, Barry S

Get full text

Molecular and Pharmacological Properties of a Potent and Selective Novel Nonsteroidal Progesterone Receptor Agonist Tanaproget by Zhang, Zhiming, Olland, Andrea M, Zhu, Yuan, Cohen, Jeff, Berrodin, Tom, Chippari, Susan, Appavu, Chandrasekaran, Li, Shen, Wilhem, James, Chopra, Raj, Fensome, Andrew, Zhang, Puwen, Wrobel, Jay, Unwalla, Rayomand J, Lyttle, C Richard, Winneker, Richard C

“…Progesterone receptor (PR) agonists have several important applications in women's health, such as in oral contraception and post-menopausal hormone therapy…”
Get full text

Molecular determinants of ERα and ERβ involved in selectivity of 16α-iodo-17β estradiol by Bhat, Ramesh A, Stauffer, Barbara, Unwalla, Rayomand J, Xu, Zhangbao, Harris, Heather A, Komm, Barry S

“…The two known estrogen receptors, ERα and ERβ, are hormone inducible transcription factors that have distinct roles in regulating cell proliferation and…”
Get full text

6-Azasteroids : potent dual inhibitors of human type 1 and 2 steroid 5α-reductase by FRYE, S. V, HAFFNER, C. D, VAN ARNOLD, J, BICKETT, D. M, MOSS, M. L, GAOCHOA TIAN, UNWALLA, R. J, LEE, F. W, TIPPIN, T. K, JMAES, M. K, GRIZZLE, M. K, JAMES, M. K, MALONEY, P. R, SCHUSTER, S. V, MOOK, R. A, DORSEY, G. F, HINER, R. N, BATCHELOR, K. W, BRAMSON, H. N, STUART, J. D, SCHWEIKER, S. L

Get full text

Understanding the Selectivity of Genistein for Human Estrogen Receptor-β Using X-Ray Crystallography and Computational Methods by Manas, Eric S., Xu, Zhang B., Unwalla, Rayomand J., Somers, William S.

“…We present X-ray crystallographic and molecular modeling studies of estrogen receptors-α and -β complexed with the estrogen receptor-β-selective phytoestrogen…”
Get full text

Structure-Based Design of Estrogen Receptor-β Selective Ligands by Manas, Eric S, Unwalla, Rayomand J, Xu, Zhang B, Malamas, Michael S, Miller, Chris P, Harris, Heather A, Hsiao, Chulai, Akopian, Tatos, Hum, Wah-Tung, Malakian, Karl, Wolfrom, Scott, Bapat, Ashok, Bhat, Ramesh A, Stahl, Mark L, Somers, William S, Alvarez, Juan C

“…We present the structure-based optimization of a series of estrogen receptor-β (ERβ) selective ligands. X-ray cocrystal structures of these ligands complexed…”
Get full text

Preparation of (.alpha.,.alpha.-dichlorobenzyl)silanes and (.alpha.-halobenzyl)silanes by Larson, Gerald L, Cartledge, Frank K, Nunez, Roberto, Unwalla, Rayomand J, Klesse, Ricardo, Del Valle, Luis

Get full text

Synthesis and Structure−Activity Relationship of Novel 6-Aryl-1,4- dihydrobenzo[d][1,3]oxazine-2-thiones as Progesterone Receptor Modulators Leading to the Potent and Selective Nonsteroidal Progesterone Receptor Agonist Tanaproget by Fensome, Andrew, Bender, Reinhold, Chopra, Rajiv, Cohen, Jeff, Collins, Mark A, Hudak, Valerie, Malakian, Karl, Lockhead, Susan, Olland, Andrea, Svenson, Kristine, Terefenko, Eugene A, Unwalla, Ray J, Wilhelm, James M, Wolfrom, Scott, Zhu, Yuan, Zhang, Zhiming, Zhang, Puwen, Winneker, Richard C, Wrobel, Jay

“…Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently…”
Get full text

Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones by McDevitt, Robert E., Malamas, Michael S., Manas, Eric S., Unwalla, Rayomand J., Xu, Zhang B., Miller, Chris P., Harris, Heather A.

“…[Display omitted] The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERβ and ERα are described. Several compounds exhibited high potency and…”
Get full text

A new generation of progesterone receptor modulators by Winneker, Richard C., Fensome, Andrew, Zhang, Puwen, Yudt, Matthew R., McComas, Casey C., Unwalla, Rayomond J.

“…Progesterone receptor (PR) modulators have evolved both structurally and mechanistically over the past half-century. Classical steroidal PR agonists continue…”
Get full text

Novel pyrrole-containing progesterone receptor modulators by COLLINS, Mark A, HUDAK, Valerie, UNWALLA, Rayomond J, WROBEL, Jay, BENDER, Reinhold, FENSOME, Andrew, PUWEN ZHANG, MILLER, Lori, WINNEKER, Richard C, ZHIMING ZHANG, YUAN ZHU, COHEN, Jeffrey

“…A series of 1,4-dihydro-2H-[d][3,1]-benzoxazin-2-one and 1,3-dihydro-[3H]-indol-2-one containing 6- or 5-, respectively, appended substituted pyrrole moieties…”
Get full text

7-Substituted 2-phenyl-benzofurans as ERβ selective ligands by Collini, Michael D., Kaufman, David H., Manas, Eric S., Harris, Heather A., Henderson, Ruth A., Xu, Zhang B., Unwalla, Rayomand J., Miller, Chris P.

“…Substituted benzofuran 21 is a potent and selective ER ligand. A series of 2-(4-hydroxy-phenyl)-benzofuran-5-ols with relatively lipophilic groups in the…”
Get full text

Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent by Frye, S V, Haffner, C D, Maloney, P R, Hiner, R N, Dorsey, G F, Noe, R A, Unwalla, R J, Batchelor, K W, Bramson, H N, Stuart, J D

“…A variety of C17 amide-substituted 6-azaandrost-4-en-3-ones were prepared and tested versus human type 1 and 2 steroid 5 alpha-reductase (5AR) and human…”
Get full text

A force field (MM2) study of 1,2-di-tert-butyl- and 1,2-disilylcyclohexanes by Unwalla, Rayomand J, Profeta, Salvatore, Cartledge, Frank K

Get full text

Structure-activity relationships for inhibition of type 1 and 2 human 5α-reductase and human adrenal 3β-hydroxy-Δ5-steroid dehydrogenase/3-keto-Δ5-steroid isomerase by 6-azaandrost-4-en-3-ones : optimization of the C17 substituent by FRYE, S. V, HAFFNER, C. D, SCHWEIKER, S. L, VAN ARNOLD, J, BICKETT, D. M, MOSS, M. L, GAOCHOA TIAN, LEE, F. W, TIPPIN, T. K, JAMES, M. K, GRIZZLE, M. K, LONG, J. E, MALONEY, P. R, CROOM, D. K, HINER, R. N, DORSEY, G. F, NOE, R. A, UNWALLA, R. J, BATCHELOR, K. W, BRAMSON, H. N, STUART, J. D

Get full text

6-Azasteroids : structure-activity relationships for inhibition of type 1 and 2 human 5α-reductase and human adrenal 3β-hydroxy-Δ5-steroid dehydrogenase/3-keto-Δ5-steroid isomerase by FRYE, S. V, HAFFNER, C. D, BATCHELOR, K. W, BRAMSON, H. N, STUART, J. D, SCHWEIKER, S. L, VAN ARNOLD, J, CROOM, S, BICKETT, D. M, MOSS, M. L, TIAN, G, UNWALLA, R. J, MALONEY, P. R, LEE, F. W, TIPPIN, T. K, JAMES, M. K, GRIZZLE, M. K, LONG, J. E, SCHUSTER, S. V, MOOK, R. A, DORSEY, G. F, HINER, R. N, CRIBBS, C. M, WHEELER, T. N, RAY, J. A, ANDREWS, R. C

Get full text

Structure and torsional potential function of allylsilane: results from MM2 and ab initio calculations [3-21G()] by Profeta, Salvatore, Unwalla, Rayomand J, Cartledge, Frank K

Get full text

Exploratory analysis of chemical structure, bacterial mutagenicity and rodent tumorigenicity by Young, S.Stanley, Profeta, Salvatore, Unwalla, Raymond J, Kosh, Joseph W

“…There are a great number of chemical compounds in use by humans and there are very limited resources for testing those compounds for potential toxicity. We…”
Get full text