Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor
MALLON, Robert, FELDBERG, Larry R, HOLLANDER, Irwin, LUCAS, Judy, CHAUDHARY, Inder, DEHNHARDT, Christoph, DELOS SANTOS, Efren, ZECHENG CHEN, DOS SANTOS, Osvaldo, AYRAL-KALOUSTIAN, Semiramis, VENKATESAN, Aranapakam
Published in Clinical cancer research (15.05.2011)
Published in Clinical cancer research (15.05.2011)
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Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin
KER YU, TORAL-BARZA, Lourdes, COLE, Derek C, ELLINGBOE, John, AYRAL-KALOUSTIAN, Semiramis, MANSOUR, Tarek S, GIBBONS, James J, ABRAHAM, Robert T, NOWAK, Pawel, ZASK, Arie, SHI, Celine, ZHANG, Wei-Guo, LUCAS, Judy, SHOR, Boris, KIM, Jamie, VERHEIJEN, Jeroen, CURRAN, Kevin, MALWITZ, David J
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Published in Cancer research (Chicago, Ill.) (01.08.2009)
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Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2
KER YU, SHI, Celine, SUNG KYOO KIM, CONANT, Roger, CURRAN, Kevin, KAPLAN, Joshua, VERHEIJEN, Jeroen, AYRAL-KALOUSTIAN, Semiramis, MANSOUR, Tarek S, ABRAHAM, Robert T, ZASK, Arie, GIBBONS, James J, TORAL-BARZA, Lourdes, LUCAS, Judy, SHOR, Boris, JAE EUN KIM, ZHANG, Wei-Guo, MAHONEY, Robert, GAYDOS, Christine, TARDIO, Luanna
Published in Cancer research (Chicago, Ill.) (15.01.2010)
Published in Cancer research (Chicago, Ill.) (15.01.2010)
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Bis(morpholino-1,3,5-triazine) Derivatives: Potent Adenosine 5′-Triphosphate Competitive Phosphatidylinositol-3-kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of Compound 26 (PKI-587), a Highly Efficacious Dual Inhibitor
Venkatesan, Aranapakam M, Dehnhardt, Christoph M, Delos Santos, Efren, Chen, Zecheng, Dos Santos, Osvaldo, Ayral-Kaloustian, Semiramis, Khafizova, Gulnaz, Brooijmans, Natasja, Mallon, Robert, Hollander, Irwin, Feldberg, Larry, Lucas, Judy, Yu, Ker, Gibbons, James, Abraham, Robert T, Chaudhary, Inder, Mansour, Tarek S
Published in Journal of medicinal chemistry (25.03.2010)
Published in Journal of medicinal chemistry (25.03.2010)
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Hybrid Inhibitors of Phosphatidylinositol 3-Kinase (PI3K) and the Mammalian Target of Rapamycin (mTOR): Design, Synthesis, and Superior Antitumor Activity of Novel Wortmannin−Rapamycin Conjugates
Ayral-Kaloustian, Semiramis, Gu, Jianxin, Lucas, Judy, Cinque, Michael, Gaydos, Christine, Zask, Arie, Chaudhary, Inder, Wang, Jianyao, Di, Li, Young, Mairead, Ruppen, Mark, Mansour, Tarek S, Gibbons, James J, Yu, Ker
Published in Journal of medicinal chemistry (14.01.2010)
Published in Journal of medicinal chemistry (14.01.2010)
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Synthesis and SAR of 6-chloro-4-fluoroalkylamino-2-heteroaryl-5-(substituted)phenylpyrimidines as anti-cancer agents
Zhang, Nan, Ayral-Kaloustian, Semiramis, Nguyen, Thai, Hernandez, Richard, Lucas, Judy, Discafani, Carolyn, Beyer, Carl
Published in Bioorganic & medicinal chemistry (2009)
Published in Bioorganic & medicinal chemistry (2009)
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Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies
Niu, Chuansheng, Ho, Douglas M., Zask, Arie, Ayral-Kaloustian, Semiramis
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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microtubule-active antitumor compound TTI-237 has both paclitaxel-like and vincristine-like properties
Beyer, Carl F, Zhang, Nan, Hernandez, Richard, Vitale, Danielle, Nguyen, Thai, Ayral-Kaloustian, Semiramis, Gibbons, James J
Published in Cancer chemotherapy and pharmacology (01.09.2009)
Published in Cancer chemotherapy and pharmacology (01.09.2009)
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Stereoselective Synthesis of an Active Metabolite of the Potent PI3 Kinase Inhibitor PKI-179
Chen, Zecheng, Venkatesan, Aranapakam M, Dos Santos, Osvaldo, Delos Santos, Efren, Dehnhardt, Christoph M, Ayral-Kaloustian, Semiramis, Ashcroft, Joseph, McDonald, Leonard A, Mansour, Tarek S
Published in Journal of organic chemistry (05.03.2010)
Published in Journal of organic chemistry (05.03.2010)
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PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors
Yu, Ker, Lucas, Judy, Zhu, Tianmin, Zask, Arie, Gaydos, Christine, Toral-Barza, Lourdes, Gu, Jianxin, Li, Fangbiao, Chaudhary, Inder, Cai, Ping, Lotvin, Jason, Petersen, Roseann, Ruppen, Mark, Fawzi, Mahdi, Ayral-Kaloustian, Semiramis, Skotnicki, Jerauld, Mansour, Tarek, Frost, Philip, Gibbons, James
Published in Cancer biology & therapy (01.05.2005)
Published in Cancer biology & therapy (01.05.2005)
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Protein Farnesyltransferase Inhibitors
AYRAL-KALOUSTIAN, Semiramis, SALASKI, Edward J
Published in Current medicinal chemistry (01.05.2002)
Published in Current medicinal chemistry (01.05.2002)
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Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in α-tubulin
Loganzo, Frank, Hari, Malathi, Annable, Tami, Tan, Xingzhi, Morilla, Daniel B, Musto, Sylvia, Zask, Arie, Kaplan, Joshua, Minnick, Jr, Albert A, May, Michael K, Ayral-Kaloustian, Semiramis, Poruchynsky, Marianne S, Fojo, Tito, Greenberger, Lee M
Published in Molecular cancer therapeutics (01.10.2004)
Published in Molecular cancer therapeutics (01.10.2004)
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Synthesis and SAR of [1,2,4]Triazolo[1,5-a]pyrimidines, a Class of Anticancer Agents with a Unique Mechanism of Tubulin Inhibition
Zhang, Nan, Ayral-Kaloustian, Semiramis, Nguyen, Thai, Afragola, Jay, Hernandez, Richard, Lucas, Judy, Gibbons, James, Beyer, Carl
Published in Journal of medicinal chemistry (25.01.2007)
Published in Journal of medicinal chemistry (25.01.2007)
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Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors
Zask, Arie, Kaplan, Joshua, Verheijen, Jeroen C, Richard, David J, Curran, Kevin, Brooijmans, Natasja, Bennett, Eric M, Toral-Barza, Lourdes, Hollander, Irwin, Ayral-Kaloustian, Semiramis, Yu, Ker
Published in Journal of medicinal chemistry (24.12.2009)
Published in Journal of medicinal chemistry (24.12.2009)
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ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines
Zask, Arie, Verheijen, Jeroen C, Curran, Kevin, Kaplan, Joshua, Richard, David J, Nowak, Pawel, Malwitz, David J, Brooijmans, Natasja, Bard, Joel, Svenson, Kristine, Lucas, Judy, Toral-Barza, Lourdes, Zhang, Wei-Guo, Hollander, Irwin, Gibbons, James J, Abraham, Robert T, Ayral-Kaloustian, Semiramis, Mansour, Tarek S, Yu, Ker
Published in Journal of medicinal chemistry (27.08.2009)
Published in Journal of medicinal chemistry (27.08.2009)
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Synthesis and SAR of Novel 4-Morpholinopyrrolopyrimidine Derivatives as Potent Phosphatidylinositol 3-Kinase Inhibitors
Chen, Zecheng, Venkatesan, Aranapakam M, Dehnhardt, Christoph M, Ayral-Kaloustian, Semiramis, Brooijmans, Natasja, Mallon, Robert, Feldberg, Larry, Hollander, Irwin, Lucas, Judy, Yu, Ker, Kong, Fangming, Mansour, Tarek S
Published in Journal of medicinal chemistry (22.04.2010)
Published in Journal of medicinal chemistry (22.04.2010)
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Lead Optimization of N-3-Substituted 7-Morpholinotriazolopyrimidines as Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of PKI-402
Dehnhardt, Christoph M, Venkatesan, Aranapakam M, Delos Santos, Efren, Chen, Zecheng, Santos, Osvaldo, Ayral-Kaloustian, Semiramis, Brooijmans, Natasja, Mallon, Robert, Hollander, Irwin, Feldberg, Larry, Lucas, Judy, Chaudhary, Inder, Yu, Ker, Gibbons, Jay, Abraham, Robert, Mansour, Tarek S
Published in Journal of medicinal chemistry (28.01.2010)
Published in Journal of medicinal chemistry (28.01.2010)
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Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent
Curran, Kevin J., Verheijen, Jeroen C., Kaplan, Joshua, Richard, David J., Toral-Barza, Lourdes, Hollander, Irwin, Lucas, Judy, Ayral-Kaloustian, Semiramis, Yu, Ker, Zask, Arie
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
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TTI-237 : A Novel Microtubule-Active Compound with In vivo Antitumor Activity
BEYER, Carl F, NAN ZHANG, HERNANDEZ, Richard, VITALE, Danielle, LUCAS, Judy, NGUYEN, Thai, DISCAFANI, Carolyn, AYRAL-KALOUSTIAN, Semiramis, GIBBONS, James J
Published in Cancer research (Chicago, Ill.) (01.04.2008)
Published in Cancer research (Chicago, Ill.) (01.04.2008)
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