Anticancer Activity of CX-3543: A Direct Inhibitor of rRNA Biogenesis
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
Published in Cancer research (Chicago, Ill.) (01.10.2009)
Published in Cancer research (Chicago, Ill.) (01.10.2009)
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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
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
Published in Journal of medicinal chemistry (27.01.2011)
Published in Journal of medicinal chemistry (27.01.2011)
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Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer
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
Published in Molecular and cellular biochemistry (01.10.2011)
Published in Molecular and cellular biochemistry (01.10.2011)
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Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics
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
Published in ACS medicinal chemistry letters (12.07.2012)
Published in ACS medicinal chemistry letters (12.07.2012)
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Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor
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
Published in ACS medicinal chemistry letters (09.02.2012)
Published in ACS medicinal chemistry letters (09.02.2012)
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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
Fellows, Ingrid M, Schwaebe, Michael, Dexheimer, Thomas S, Vankayalapati, Hariprasad, Gleason-Guzman, Mary, Whitten, Jeffrey P, Hurley, Laurence H
Published in Molecular cancer therapeutics (01.11.2005)
Published in Molecular cancer therapeutics (01.11.2005)
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Design and Synthesis of a Series of Non-Peptide High-Affinity Human Corticotropin-Releasing Factor1 Receptor Antagonists
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
Published in Journal of medicinal chemistry (25.10.1996)
Published in Journal of medicinal chemistry (25.10.1996)
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Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor1 (CRF1) receptor antagonists
HUANG, Charles Q, GRIGORIADIS, Dimitri E, ZHENGYU LIU, MCCARTHY, James R, RAMPHAL, John, WEBB, Thomas, WHITTEN, Jeffrey P, XIE, Michael Y, CHEN CHEN
Published in Bioorganic & medicinal chemistry letters (03.05.2004)
Published in Bioorganic & medicinal chemistry letters (03.05.2004)
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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
Whitten, Jeffrey P, Xie, Yun Feng, Erickson, Philip E, Webb, Thomas R, De Souza, Errol B, Grigoriadis, Dimitri E, McCarthy, James R
Published in Journal of medicinal chemistry (25.10.1996)
Published in Journal of medicinal chemistry (25.10.1996)
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Abstract 1319: Repotrectinib, a new generation ROS1 inhibitor, is highly potent against fusion ROS1s and emerging resistance mutations
Deng, Wei, Zhai, Dayong, Zhang, Xin, Lee, Dong, Rogers, Evan, Whitten, Jeffrey, Cui, J. Jean
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Abstract 4796: Ropotrectinib is a novel polypharmacology kinase inhibitor against WT and mutant ROS1, TRK and ALK
Deng, Wei, Zhai, Dayong, Huang, John, Rogers, Evan, Whitten, Jeffrey, Lim, John, Li, Yishan, Cui, Jean
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Abstract 2133: Ending the endless acquired tyrosine kinase resistance mutations — Design of TPX-0005, a multi-target ALK/ROS1/TRK inhibitor with broad spectrum activity against wild-type and mutants including ALK G1202R, ROS1 G2032R and TRKA G595R
Cui, J. Jean, Rogers, Evan, Zhai, Dayong, Deng, Wei, Huang, Zhongdong, Whitten, Jeffrey, Li, Yishan
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Abstract 2133: Ending the endless acquired tyrosine kinase resistance mutations Design of TPX-0005, a multi-target ALKROS1TRK inhibitor with broad spectrum activity against wild-type and mutants including ALK G1202R, ROS1 G2032R and TRKA G595R
Cui, JJean, Rogers, Evan, Zhai, Dayong, Deng, Wei, Huang, Zhongdong, Whitten, Jeffrey, Li, Yishan
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Abstract B186: TPX-0005, a polypharmacology inhibitor, overcomes ALK treatment resistance from acquired mutations, bypass signaling, and EMT
Zhai, Dayong, Deng, Wei, Rogers, Evan, Huang, Zhongdong, Whitten, Jeffrey, Lim, John, Li, Yishan, Cui, J. Jean
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Abstract B185: TPX-0005, a supreme ROS1 inhibitor, overcomes crizotinib-resistant ROS1 mutations including solvent front mutation G2032R and gatekeeper mutation L2026M
Cui, J. Jean, Zhai, Dayong, Deng, Wei, Rogers, Evan, Huang, Zhongdong, Whitten, Jeffrey, Lim, John, Li, Yishan
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Abstract B184: TPX-0005, a highly potent TRK inhibitor, effectively overcomes clinical-resistance TRK mutations including solvent front mutants TRKA G595R, TRKB G639R, and TRKC G623R
Cui, J. Jean, Zhai, Dayong, Deng, Wei, Rogers, Evan, Huang, Zhongdong, Whitten, Jeffrey, lim, John, Li, Yishan
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Abstract 1321: TPX-0022, a polypharmacology inhibitor of MET/CSF1R/SRC for treatment of cancers with abnormal HGF/MET signaling
Zhai, Dayong, Rogers, Evan, Deng, Wei, Zhang, Xin, Lee, Dong, Ung, Jane, Zhang, Han, Liu, Jing, Lu, Yuelie, Huang, John, Graber, Armin, Zimmerman, Zach, Lim, John, Whitten, Jeffrey, Cui, J. Jean
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Abstract 1325: TPX-0022, a polypharmacology inhibitor of MET/CSF1R/SRC inhibits tumor growth by promoting anti-tumor immune responses
Deng, Wei, Zhai, Dayong, Rogers, Evan, Zhang, Xin, Lee, Dong, Ung, Jane, Zhang, Han, Liu, Jing, Lu, Yuelie, Huang, John, Graber, Armin, Zimmerman, Zach, Lim, John, Whitten, Jeffrey, Cui, J. Jean
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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