Search Results - "Heyman, H. Robin"

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases by Curtin, Michael L., Robin Heyman, H., Frey, Robin R., Marcotte, Patrick A., Glaser, Keith B., Jankowski, James R., Magoc, Terrance J., Albert, Daniel H., Olson, Amanda M., Reuter, David R., Bouska, Jennifer J., Montgomery, Debra A., Palma, Joann P., Donawho, Cherrie K., Stewart, Kent D., Tse, Chris, Michaelides, Michael R.

“…A series of pyrazole diaminopyrimidines with dual KDR/Aurora B kinase inhibitory activity has been identified. The SAR, physiochemical properties and antitumor…”
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Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families by Curtin, Michael L., Frey, Robin R., Heyman, H. Robin, Soni, Niru B., Marcotte, Patrick A., Pease, Lori J., Glaser, Keith B., Magoc, Terrance J., Tapang, Paul, Albert, Daniel H., Osterling, Donald J., Olson, Amanda M., Bouska, Jennifer J., Guan, Zhiwen, Preusser, Lee C., Polakowski, James S., Stewart, Kent D., Tse, Chris, Davidsen, Steven K., Michaelides, Michael R.

“…A series of thienopyridine ureas with dual inhibitory activity against KDR and Aurora B kinase has been identified. Compound 2 (ABT-348) of this series is…”
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Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors by Wilsbacher, Julie L, Cheng, Min, Cheng, Dong, Trammell, Samuel A J, Shi, Yan, Guo, Jun, Koeniger, Stormy L, Kovar, Peter J, He, Yupeng, Selvaraju, Sujatha, Heyman, H Robin, Sorensen, Bryan K, Clark, Richard F, Hansen, T Matthew, Longenecker, Kenton L, Raich, Diana, Korepanova, Alla V, Cepa, Steven, Towne, Danli L, Abraham, Vivek C, Tang, Hua, Richardson, Paul L, McLoughlin, Shaun M, Badagnani, Ilaria, Curtin, Michael L, Michaelides, Michael R, Maag, David, Buchanan, F Gregory, Chiang, Gary G, Gao, Wenqing, Rosenberg, Saul H, Brenner, Charles, Tse, Chris

“…Cancer cells are highly reliant on NAD -dependent processes, including glucose metabolism, calcium signaling, DNA repair, and regulation of gene expression…”
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SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT) by Curtin, Michael L., Heyman, H. Robin, Clark, Richard F., Sorensen, Bryan K., Doherty, George A., Hansen, T. Matthew, Frey, Robin R., Sarris, Kathy A., Aguirre, Ana L., Shrestha, Anurupa, Tu, Noah, Woller, Kevin, Pliushchev, Marina A., Sweis, Ramzi F., Cheng, Min, Wilsbacher, Julie L., Kovar, Peter J., Guo, Jun, Cheng, Dong, Longenecker, Kenton L., Raich, Diana, Korepanova, Alla V., Soni, Nirupama B., Algire, Mikkel A., Richardson, Paul L., Marin, Violeta L., Badagnani, Ilaria, Vasudevan, Anil, Buchanan, F. Greg, Maag, David, Chiang, Gary G., Tse, Chris, Michaelides, Michael R.

“…[Display omitted] Herein we disclose SAR studies that led to a series of isoindoline ureas which we recently reported were first-in-class, non-substrate…”
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Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC) by CURTIN, Michael L, GARLAND, Robert B, HEYMAN, H. Robin, FREY, Robin R, MICHAELIDES, Michael R, JUNLING LI, PEASE, Lori J, GLASER, Keith B, MARCOTTE, Patrick A, DAVIDSEN, Steven K

“…A series of succinimide hydroxamic acids was prepared and evaluated in vitro for HDAC inhibition and tumor cell antiproliferation. While the original…”
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Thienopyridine urea inhibitors of KDR kinase by Heyman, H. Robin, Frey, Robin R., Bousquet, Peter F., Cunha, George A., Moskey, Maria D., Ahmed, Asma A., Soni, Niru B., Marcotte, Patrick A., Pease, Lori J., Glaser, Keith B., Yates, Melinda, Bouska, Jennifer J., Albert, Daniel H., Black-Schaefer, Candace L., Dandliker, Peter J., Stewart, Kent D., Rafferty, Paul, Davidsen, Steven K., Michaelides, Michael R., Curtin, Michael L.

“…The evaluation of KDR kinase inhibitor 2 (IC 50 = 9 nM) and related analogs is reported. A series of substituted thienopyridine ureas was prepared and…”
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Phenoxyphenyl Sulfone N-Formylhydroxylamines (Retrohydroxamates) as Potent, Selective, Orally Bioavailable Matrix Metalloproteinase Inhibitors by Wada, Carol K, Holms, James H, Curtin, Michael L, Dai, Yujia, Florjancic, Alan S, Garland, Robert B, Guo, Yan, Heyman, H. Robin, Stacey, Jamie R, Steinman, Douglas H, Albert, Daniel H, Bouska, Jennifer J, Elmore, Ildiko N, Goodfellow, Carole L, Marcotte, Patrick A, Tapang, Paul, Morgan, Douglas W, Michaelides, Michael R, Davidsen, Steven K

“…A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated as matrix metalloproteinases (MMP) inhibitors. The substitution of…”
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Heterocyclic ketones as inhibitors of histone deacetylase by Vasudevan, Anil, Ji, Zhiqin, Frey, Robin R., Wada, Carol K., Steinman, Douglas, Heyman, H.Robin, Guo, Yan, Curtin, Michael L., Guo, Jun, Li, Junling, Pease, Lori, Glaser, Keith B., Marcotte, Patrick A., Bouska, Jennifer J., Davidsen, Steven K., Michaelides, Michael R.

“…Several heterocyclic ketones were investigated as potential inhibitors of histone deacetylase. Nanomolar inhibitors such as 22 and 25 were obtained, the…”
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Isoindolinone ureas: a novel class of KDR kinase inhibitors by Curtin, Michael L, Frey, Robin R, Heyman, H.Robin, Sarris, Kathy A, Steinman, Douglas H, Holmes, James H, Bousquet, Peter F, Cunha, George A, Moskey, Maria D, Ahmed, Asma A, Pease, Lori J, Glaser, Keith B, Stewart, Kent D, Davidsen, Steven K, Michaelides, Michael R

“…The evaluation of KDR kinase inhibitor 4e (IC 50 7 nM) and related analogs is reported. A series of substituted isoindolinone ureas was prepared and evaluated…”
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Biaryl Ether Retrohydroxamates as Potent, Long-lived, Orally Bioavailable MMP Inhibitors by Michaelides, Michael R., Dellaria, Joseph F., Gong, Jane, Holms, James H., Bouska, Jennifer J., Stacey, Jamie, Wada, Carol K., Heyman, H.Robin, Curtin, Michael L., Guo, Yan, Goodfellow, Carole L., Elmore, Ildiko B., Albert, Daniel H., Magoc, Terrance J., Marcotte, Patrick A., Morgan, Douglas W., Davidsen, Steven K.

“…A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against…”
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Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770 by Curtin, Michael L., Florjancic, Alan S., Heyman, H.Robin, Michaelides, Michael R., Garland, Robert B., Holms, James H., Steinman, Douglas H., Dellaria, Joseph F., Gong, Jane, Wada, Carol K., Guo, Yan, Elmore, Ildiko B., Tapang, Paul, Albert, Daniel H., Magoc, Terrance J., Marcotte, Patrick A., Bouska, Jennifer J., Goodfellow, Carole L., Bauch, Joy L., Marsh, Kennan C., Morgan, Douglas W., Davidsen, Steven K.

“…Modification of the biphenyl portion of MMP inhibitor 2a gave analogue 2i which is greater than 1000-fold selective against MMP-2 versus MMP-1. The…”
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Discovery and Evaluation of a Series of 3-Acylindole Imidazopyridine Platelet-Activating Factor Antagonists by Curtin, Michael L, Davidsen, Steven K, Heyman, H. Robin, Garland, Robert B, Sheppard, George S, Florjancic, Alan S, Xu, Lianhong, Carrera, George M, Steinman, Douglas H, Trautmann, Jeff A, Albert, Daniel H, Magoc, Terrance J, Tapang, Paul, Rhein, David A, Conway, Richard G, Luo, Gongjin, Denissen, Jon F, Marsh, Kennan C, Morgan, Douglas W, Summers, James B

“…Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and…”
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N-(Acyloxyalkyl)pyridinium Salts as Soluble Prodrugs of a Potent Platelet Activating Factor Antagonist by Davidsen, Steven K, Summers, James B, Albert, Daniel H, Holms, James H, Heyman, H. Robin, Magoc, Terrance J, Conway, Richard G, Rhein, David A, Carter, George W

“…Pyrrolothiazole 4 is a potent antagonist of platelet activating factor-mediated effects in a variety of in vitro and in vivo assays. Despite its positive…”
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The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors by Steinman, Douglas H., Curtin, Michael L., Garland, Robert B., Davidsen, Steven K., Heyman, H.Robin, Holms, James H., Albert, Daniel H., Magoc, Terry J., Nagy, Ildiko B., Marcotte, Patrick A., Li, Junling, Morgan, Douglas W., Hutchins, Charles, Summers, James B.

“…A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were designed, synthesized, and evaluated as inhibitors of matrix…”
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Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist by Albert, Daniel H., Magoc, Terrance J., Tapang, Paul, Luo, Gongjin, Morgan, Douglas W., Curtin, Michael, Sheppard, George S., Xu, Lianhong, Heyman, H.Robin, Davidsen, Steven K., Summers, James B., Carter, George W.

“…ABT-491 (4-ethynyl- N, N-dimethyl-3-[3-fluoro-4-[(2-methyl-1 H-imidazo-[4,5- c]pyridin-1-yl)methyl]benzoyl]-1 H-indole-1-carboxamide hydrochloride) is a novel…”
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3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a Novel Series of Platelet Activating Factor Antagonists by Sheppard, George S, Pireh, Daisy, Carrera, George M, Bures, Mark G, Heyman, H. Robin, Steinman, Douglas H, Davidsen, Steven K, Phillips, James G, Guinn, Denise E, May, Paul D, Conway, Richard D, Rhein, David A, Calhoun, William C, Albert, Daniel H, Magoc, Terrance J, Carter, George W, Summers, James B

“…(2RS,4R)-3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles represent a new class of potent, orally active antagonists of platelet activating factor (PAF). The…”
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Evaluation of the inhibition of other metalloproteinases by matrix metalloproteinase inhibitors by Marcotte, P A, Elmore, I N, Guan, Z, Magoc, T J, Albert, D H, Morgand, D W, Curtin, M L, Garland, R B, Guo, Y, Heyman, H R, Holms, J H, Sheppard, G S, Steinman, D H, Wada, C K, Davidsen, S K

“…Two series of compounds synthesized as specific matrix metalloproteinase (MMP) inhibitors have been evaluated for their inhibition of non-MMPs. In a series of…”
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Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists by Guinn, Denise E, Summers, James B, Heyman, H. Robin, Conway, Richard G, Rhein, David A, Albert, Daniel H, Magoc, Terry, Carter, George W

“…A class of N-substituted tetrahydrobenzopyrano[3,4-c]pyridines, I, have been identified as antagonists of platelet activating factor (PAF). The structural…”
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Synthesis and evaluation of water soluble indole pyrrolothiazole paf antagonists by Sheppard, George S., Davidsen, Steven K., Carrera, George M., Pireh, Daisy, Holms, James H., Robin Heyman, H., Steinman, Douglas H., Curtin, Michael L., Conway, Richard G., Rhein, David A., Albert, Daniel H., Tapang, Paul, Magoc, Terrance J., Summers, James B.

“…3-(3-Pyridinyl)-7-(indol-3-ylcarbonyl)-1 H-3 H-pyrrolo[1,2-c]thiazoles represent a class of potent, orally active PAF antagonists; however, the lead compounds…”
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Discovery and optimization of indole pyrrolothiazole paf antagonists by Holms, James H., Davidsen, Steven K., Sheppard, George S., Carrera, George M., Curtin, Nichael L., Heyman, H.Robin, Pireh, Daisy, Steinman, Douglas H., Albert, Daniel H., Conway, Richard G., Luo, Gongjin, Magoc, Terrance J., Tapang, Paul, Rhein, David A., Summers, James B.

“…3-(3-Pyridinyl)-7-(indol-3-ylcarbonyl)-1 H-3 H-pyrrolo[1,2-c]thiazoles represent a new class of platelet activating factor antagonists. This series was…”
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