Search Results - "WHITTEN, Jeffrey P"

Anticancer Activity of CX-3543: A Direct Inhibitor of rRNA Biogenesis by DRYGIN, Denis, SIDDIQUI-JAIN, Adam, LIM, John K. C, VON HOFF, Daniel, ANDERES, Kenna, RICE, William G, O'BRIEN, Sean, SCHWAEBE, Michael, LIN, Amy, BLIESATH, Josh, HO, Caroline B, PROFFITT, Chris, TRENT, Katy, WHITTEN, Jeffrey P

“…Hallmark deregulated signaling in cancer cells drives excessive ribosome biogenesis within the nucleolus, which elicits unbridled cell growth and…”
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Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the Treatment of Cancer by Pierre, Fabrice, Chua, Peter C, O’Brien, Sean E, Siddiqui-Jain, Adam, Bourbon, Pauline, Haddach, Mustapha, Michaux, Jerome, Nagasawa, Johnny, Schwaebe, Michael K, Stefan, Eric, Vialettes, Anne, Whitten, Jeffrey P, Chen, Ta Kung, Darjania, Levan, Stansfield, Ryan, Anderes, Kenna, Bliesath, Josh, Drygin, Denis, Ho, Caroline, Omori, May, Proffitt, Chris, Streiner, Nicole, Trent, Katy, Rice, William G, Ryckman, David M

“…Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-competitive inhibitor of protein kinase CK2 in clinical trials…”
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Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer by Pierre, Fabrice, Chua, Peter C., O’Brien, Sean E., Siddiqui-Jain, Adam, Bourbon, Pauline, Haddach, Mustapha, Michaux, Jerome, Nagasawa, Johnny, Schwaebe, Michael K., Stefan, Eric, Vialettes, Anne, Whitten, Jeffrey P., Chen, Ta Kung, Darjania, Levan, Stansfield, Ryan, Bliesath, Joshua, Drygin, Denis, Ho, Caroline, Omori, May, Proffitt, Chris, Streiner, Nicole, Rice, William G., Ryckman, David M., Anderes, Kenna

“…In this article we describe the preclinical characterization of 5-(3-chlorophenylamino) benzo[ c ][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first…”
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Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics by Haddach, Mustapha, Schwaebe, Michael K, Michaux, Jerome, Nagasawa, Johnny, O'Brien, Sean E, Whitten, Jeffrey P, Pierre, Fabrice, Kerdoncuff, Pauline, Darjania, Levan, Stansfield, Ryan, Drygin, Denis, Anderes, Kenna, Proffitt, Chris, Bliesath, Josh, Siddiqui-Jain, Adam, Omori, May, Huser, Nanni, Rice, William G, Ryckman, David M

“…Accelerated proliferation of solid tumor and hematologic cancer cells is linked to accelerated transcription of rDNA by the RNA polymerase I (Pol I) enzyme to…”
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Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor by Haddach, Mustapha, Michaux, Jerome, Schwaebe, Michael K, Pierre, Fabrice, O’Brien, Sean E, Borsan, Cosmin, Tran, Joe, Raffaele, Nicholas, Ravula, Suchitra, Drygin, Denis, Siddiqui-Jain, Adam, Darjania, Levan, Stansfield, Ryan, Proffitt, Chris, Macalino, Diwata, Streiner, Nicole, Bliesath, Joshua, Omori, May, Whitten, Jeffrey P, Anderes, Kenna, Rice, William G, Ryckman, David M

“…Structure–activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases…”
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Determination of the importance of the stereochemistry of psorospermin in topoisomerase II–induced alkylation of DNA and in vitro and in vivo biological activity by Fellows, Ingrid M, Schwaebe, Michael, Dexheimer, Thomas S, Vankayalapati, Hariprasad, Gleason-Guzman, Mary, Whitten, Jeffrey P, Hurley, Laurence H

“…Psorospermin is a natural product that has been shown to have activity against drug-resistant leukemia lines and AIDS-related lymphoma. It has also been shown…”
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Design and Synthesis of a Series of Non-Peptide High-Affinity Human Corticotropin-Releasing Factor1 Receptor Antagonists by Chen, Dagnino, Raymond, De Souza, Errol B, Grigoriadis, Dimitri E, Huang, Charles Q, Kim, Kyung-Il, Liu, Zhengyu, Moran, Terry, Webb, Thomas R, Whitten, Jeffrey P, Xie, Yun Feng, McCarthy, James R

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Nickel(0)-catalyzed coupling of vinylzirconiums to α-bromo-α,α-difluoro esters. Convenient generation of a functionalized allyldifluoro moiety by Schwaebe, Michael K, McCarthy, James R, Whitten, Jeffrey P

“…Vinylzirconium reagents couple with α-bromo-α,α-difluoro esters in the presence of a Ni(PPh 3) 4 catalyst to form alkenyl difluoro esters in good yields. This…”
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Modeling of competitive phosphono amino acid NMDA receptor antagonists by Whitten, Jeffrey P, Harrison, Boyd L, Weintraub, Herschel J. R, McDonald, Ian A

“…A pharmacophore for the phosphono amino acid antagonists of the NMDA receptor has been developed using computer-based molecular modeling techniques. An…”
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Synthesis and cardiotonic activity of novel biimidazoles by Matthews, Donald P, McCarthy, James R, Whitten, Jeffrey P, Kastner, Philip R, Barney, Charlotte L, Marshall, Franklin N, Ertel, Marcia A, Burkhard, Therese, Shea, Philip J, Kariya, Takashi

“…A series of substituted 2,2'-bi-1H-imidazoles and related analogues was synthesized and evaluated for inotropic activity. Structure-activity relationship…”
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Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor1 (CRF1) receptor antagonists by HUANG, Charles Q, GRIGORIADIS, Dimitri E, ZHENGYU LIU, MCCARTHY, James R, RAMPHAL, John, WEBB, Thomas, WHITTEN, Jeffrey P, XIE, Michael Y, CHEN CHEN

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Rapid Microscale Synthesis, a New Method for Lead Optimization Using Robotics and Solution Phase Chemistry:  Application to the Synthesis and Optimization of Corticotropin-Releasing Factor1 Receptor Antagonists by Whitten, Jeffrey P, Xie, Yun Feng, Erickson, Philip E, Webb, Thomas R, De Souza, Errol B, Grigoriadis, Dimitri E, McCarthy, James R

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Facile synthesis of the four 3-aminocyclopentane-1,2-diol stereoisomers by Whitten, Jeffrey P, McCarthy, James R, Whalon, Michael R

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[2-(Trimethylsilyl)ethoxy]methyl (SEM) as a novel and effective imidazole and fused aromatic imidazole protecting group by Whitten, Jeffrey P, Matthews, Donald P, McCarthy, James R

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(R)-4-Oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex by Whitten, Jeffrey P, Baron, Bruce M, Muench, Daniel, Miller, Francis, White, H. Steven, McDonald, Ian A

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Total synthesis of psorospermin by Schwaebe, Michael K., Moran, Terence J., Whitten, Jeffrey P.

“…The xanthone natural product psorospermin was synthesized in 13 steps with an overall yield of 1.7%. This compound shows potent antineoplastic activity in a…”
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A novel and efficient synthesis of 3-carboxy-4-oxo-1,8-naphthyridines using magnesium chloride by Chua, Peter C., Nagasawa, Johnny Y., Pierre, Fabrice, Schwaebe, Michael K., Vialettes, Anne, Whitten, Jeffrey P.

“…A novel and efficient synthesis of 5-oxo-6-carboxy-naphthyridines is reported in this Letter along with a discussion of scope and limitations. Activated…”
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A convenient procedure for the preparation of 4(5)-cyanoimidazoles by Matthews, Donald P, Whitten, Jeffrey P, McCarthy, James R

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Halogenation of [2-(trimethylsilyl)ethoxy]methyl (SEM) protected 2,2′-Bi-H-imidazole by Matthews, Donald P., Whitten, Jeffrey P., Mccarthy, James R.

“…2,2′‐Bi‐1H‐imidazole, when protected with the [2‐(trimethylsilyl)ethoxy]methyl (SEM) blocking group, on treatment with N‐bromosuccinimide or…”
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1-(Thienylalkyl)imidazole-2(3H)-thiones as potent competitive inhibitors of dopamine .beta.-hydroxylase by McCarthy, James R, Matthews, Donald P, Broersma, Robert J, McDermott, Roger D, Kastner, Philip R, Hornsperger, Jean Marie, Demeter, David A, Weintraub, Herschel J. R, Whitten, Jeffrey P

“…1-(2-Thienylalkyl)imidazole-2(3H)-thiones (5a-k) are competitive inhibitors of dopamine beta-hydroxylase (DBH) and demonstrate the utility of thiophene in the…”
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