Search Results - "Hammond, Marlys"

Development of a Small-Molecule Serum-and Glucocorticoid-Regulated Kinase-1 Antagonist and Its Evaluation as a Prostate Cancer Therapeutic by SHERK, Andrea B, FRIGO, Daniel E, NORRIS, John D, MCDONNELL, Donald P, SCHNACKENBERG, Christine G, BRAY, Jeffrey D, LAPING, Nicholas J, TRIZNA, Walter, HAMMOND, Marlys, PATTERSON, Jaclyn R, THOMPSON, Scott K, KAZMIN, Dmitri

“…Androgens, through their actions on the androgen receptor (AR), are required for the development of the prostate and contribute to the pathologic growth…”
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Development of an Enantioselective Synthetic Route to Neocarzinostatin Chromophore and Its Use for Multiple Radioisotopic Incorporation by Myers, Andrew G., Glatthar, Ralf, Hammond, Marlys, Harrington, Philip M., Kuo, Elaine Y., Liang, Jun, Schaus, Scott E., Wu, Yusheng, Xiang, Jia-Ning

“…A convergent, enantioselective synthetic route to the natural product neocarzinostatin chromophore (1) is described. Synthesis of the chromophore aglycon (2)…”
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Total Synthesis of (+)-Neocarzinostatin Chromophore by Myers, Andrew G, Liang, Jun, Hammond, Marlys, Harrington, Philip M, Wu, Yusheng, Kuo, Elaine Y

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Enantioselective Synthesis of Neocarzinostatin Chromophore Aglycon by Myers, Andrew G, Hammond, Marlys, Wu, Yusheng, Xiang, Jia-Ning, Harrington, Philip M, Kuo, Elaine Y

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A Comparison of DNA Cleavage by Neocarzinostatin Chromophore and Its Aglycon:  Evaluating the Role of the Carbohydrate Residue by Myers, Andrew G, Kort, Michael E, Hammond, Marlys

“…Through a comparative analysis of the reactivity and DNA cleaving activity of neocarzinostatin (NCS) chromophore (1) and the corresponding aglycon (2), we show…”
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Identification of Purines and 7‑Deazapurines as Potent and Selective Type I Inhibitors of Troponin I‑Interacting Kinase (TNNI3K) by Lawhorn, Brian G, Philp, Joanne, Zhao, Yongdong, Louer, Christopher, Hammond, Marlys, Cheung, Mui, Fries, Harvey, Graves, Alan P, Shewchuk, Lisa, Wang, Liping, Cottom, Joshua E, Qi, Hongwei, Zhao, Huizhen, Totoritis, Rachel, Zhang, Guofeng, Schwartz, Benjamin, Li, Hu, Sweitzer, Sharon, Holt, Dennis A, Gatto, Gregory J, Kallander, Lara S

“…A series of cardiac troponin I-interacting kinase (TNNI3K) inhibitors arising from 3-((9H-purin-6-yl)­amino)-N-methyl-benzenesulfonamide (1) is disclosed along…”
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Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4) by Brooks, Carl A, Barton, Linda S, Behm, David J, Eidam, Hilary S, Fox, Ryan M, Hammond, Marlys, Hoang, Tram H, Holt, Dennis A, Hilfiker, Mark A, Lawhorn, Brian G, Patterson, Jaclyn R, Stoy, Patrick, Roethke, Theresa J, Ye, Guosen, Zhao, Steve, Thorneloe, Kevin S, Goodman, Krista B, Cheung, Mui

“…GSK2798745, a clinical candidate, was identified as an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) ion channel for the treatment of…”
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Synthetic aspects of an asymmetric nitrogen-insertion process: preparation of chiral, non-racemic caprolactams and valerolactams. Total synthesis of (-)-alloyohimbane by Aube, Jeffrey, Wang, Yuguang, Hammond, Marlys, Tanol, Mehmet, Takusagawa, Fusao, Vander Velde, David

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Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1 by Kallander, Lara S., Washburn, David, Hilfiker, Mark A., Eidam, Hilary Schenck, Lawhorn, Brian G., Prendergast, Joanne, Fox, Ryan, Dowdell, Sarah, Manns, Sharada, Hoang, Tram, Zhao, Steve, Ye, Guosen, Hammond, Marlys, Holt, Dennis A., Roethke, Theresa, Hong, Xuan, Reid, Robert A., Gampe, Robert, Zhang, Hong, Diaz, Elsie, Rendina, Alan R., Quinn, Amy M., Willette, Bob

“…Bone Morphogenetic Protein 1 (BMP1) inhibition is a potential method for treating fibrosis because BMP1, a member of the zinc metalloprotease family, is…”
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Syntheses and rearrangements of spirocyclic oxaziridines derived from unsymmetrical ketones by Aube, Jeffrey, Hammond, Marlys, Gherardini, Elyse, Takusagawa, Fusao

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Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors by Hammond, Marlys, Washburn, David G., Hoang, Tram H., Manns, Sharada, Frazee, James S., Nakamura, Hiroko, Patterson, Jaclyn R., Trizna, Walter, Wu, Charlene, Azzarano, Leonard M., Nagilla, Rakesh, Nord, Melanie, Trejo, Rebecca, Head, Martha S., Zhao, Baoguang, Smallwood, Angela M., Hightower, Kendra, Laping, Nicholas J., Schnackenberg, Christine G., Thompson, Scott K.

“…SGK1 inhibitors 1 and 2 suffered from poor oral exposure that could be attributed to factors such as high clearance and formation of glucuronic acid…”
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2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3- b]pyridine derivatives as selective progesterone receptor agonists by Wang, Yonghui, Duraiswami, Chaya, Madauss, Kevin P., Tran, Thuy B., Williams, Shawn P., Deng, Su-Jun, Graybill, Todd L., Hammond, Marlys, Jones, David G., Grygielko, Eugene T., Bray, Jeffrey D., Thompson, Scott K.

“…A novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3- b]pyridine derivatives was identified as selective PR…”
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Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: Potent, orally-active 1,4-disubstituted imidazoles by Dow, Robert L., Hadcock, John R., Scott, Dennis O., Schneider, Steven R., Paight, Ernest S., Iredale, Philip A., Carpino, Philip A., Griffith, David A., Hammond, Marlys, DaSilva-Jardine, Paul

“…A new series of CB 1 receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is…”
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Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists by Hammond, Marlys, Patterson, Jaclyn R., Manns, Sharada, Hoang, Tram H., Washburn, David G., Trizna, Walter, Glace, Lindsay, Grygielko, Eugene T., Nagilla, Rakesh, Nord, Melanie, Fries, Harvey E., Minick, Douglas J., Laping, Nicholas J., Bray, Jeffrey D., Thompson, Scott K.

“…Two series of amino acid-derived heterocyclic progesterone receptor (PR) ligands are reported. Tetrazole-containing ligands behaved as potent PR partial…”
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Improving the developability profile of pyrrolidine progesterone receptor partial agonists by Kallander, Lara S., Washburn, David G., Hoang, Tram H., Frazee, James S., Stoy, Patrick, Johnson, Latisha, Lu, Qing, Hammond, Marlys, Barton, Linda S., Patterson, Jaclyn R., Azzarano, Leonard M., Nagilla, Rakesh, Madauss, Kevin P., Williams, Shawn P., Stewart, Eugene L., Duraiswami, Chaya, Grygielko, Eugene T., Xu, Xiaoping, Laping, Nicholas J., Bray, Jeffrey D., Thompson, Scott K.

“…The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities…”
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Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists by Washburn, David G., Hoang, Tram H., Frazee, James S., Johnson, Latisha, Hammond, Marlys, Manns, Sharada, Madauss, Kevin P., Williams, Shawn P., Duraiswami, Chaya, Tran, Thuy B., Stewart, Eugene L., Grygielko, Eugene T., Glace, Lindsay E., Trizna, Walter, Nagilla, Rakesh, Bray, Jeffrey D., Thompson, Scott K.

“…We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR…”
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Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists by ELLIOTT, Richard L, OLIVER, Robert M, MACK, Christine M, CASSELLA, James V, LAFLAMME, Janet A, GILLASPY, Melissa L, HAMMOND, Marlys, HANK, Richard F, MAURER, Tristan S, BAKER, Demetria L, DASILVA-JARDINE, Paul A, STEVENSON, Ralph W

“…A series of 2-heteroaryl-4-arylimidazoles with potent in vitro activity at the NPY5 receptor was developed. Introduction of electron-withdrawing groups on the…”
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In Vitro and in Vivo Characterization of 3-{2-[6-(2-tert-Butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl}benzonitrile Hydrochloride Salt, a Potent and Selective NPY5 Receptor Antagonist by Elliott, Richard L, Oliver, Robert M, Hammond, Marlys, Patterson, Terrell A, She, Li, Hargrove, Diane M, Martin, Kelly A, Maurer, Tristan S, Kalvass, J. Cory, Morgan, Bradley P, DaSilva-Jardine, Paul A, Stevenson, Ralph W, Mack, Christine M, Cassella, James V

“…To investigate the anorectic potential of NPY5 receptor antagonists, we have profiled the in vitro and in vivo properties of…”
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In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist by Elliott, Richard L, Oliver, Robert M, Hammond, Marlys, Patterson, Terrell A, She, Li, Hargrove, Diane M, Martin, Kelly A, Maurer, Tristan S, Kalvass, J Cory, Morgan, Bradley P, DaSilva-Jardine, Paul A, Stevenson, Ralph W, Mack, Christine M, Cassella, James V

“…To investigate the anorectic potential of NPY5 receptor antagonists, we have profiled the in vitro and in vivo properties of…”
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Structure–activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles, core-modified analogues and amide isosteres by Hammond, Marlys, Elliott, Richard L., Gillaspy, Melissa L., Hager, David C., Hank, Richard F., LaFlamme, Janet A., Oliver, Robert M., DaSilva-Jardine, Paul A., Stevenson, Ralph W., Mack, Christine M., Cassella, James V.

“…Beginning with carbazole 1a, the amide and alkyl substituents were optimized to maintain potency while adding solubilizing groups. Efforts to replace the…”
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