Search Results - "DISCAFANI, Carolyn"

Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase by RABINDRAN, Sridhar K, DISCAFANI, Carolyn M, REICH, Marvin F, RU SHEN, XIAOQING SHI, TSOU, Hwei-Ru, WANG, Yu-Fen, WISSNER, Allan, ROSFJORD, Edward C, BAXTER, Michelle, FLOYD, M. Brawner, GOLAS, Jonathan, HALLETT, William A, JOHNSON, Bernard D, NILAKANTAN, Ramaswamy, OVERBEEK, Elsebe

“…HER-2 belongs to the ErbB family of receptor tyrosine kinases, which has been implicated in a variety of cancers. Overexpression of HER-2 is seen in 25-30% of…”
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Epidermal Growth Factor Receptor Variant III Mutations in Lung Tumorigenesis and Sensitivity to Tyrosine Kinase Inhibitors by Ji, Hongbin, Zhao, Xiaojun, Yuza, Yuki, Shimamura, Takeshi, Li, Danan, Protopopov, Alexei, Jung, Boonim L., McNamara, Kate, Xia, Huili, Glatt, Karen A., Thomas, Roman K., Sasaki, Hidefumi, Horner, James W., Eck, Michael, Mitchell, Albert, Sun, Yangping, Al-Hashem, Ruqayyah, Bronson, Roderick T., Rabindran, Sridhar K., Discafani, Carolyn M., Maher, Elizabeth, Shapiro, Geoffrey I., Meyerson, Matthew, Wong, Kwok-Kin

“…The tyrosine kinase inhibitors gefitinib (Iressa) and erlotinib (Tarceva) have shown anti-tumor activity in the treatment of non-small cell lung cancer…”
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Combinatorial chemoprevention of intestinal neoplasia by Frost, Philip, Torrance, Christopher J, Jackson, Peta E, Montgomery, Elizabeth, Kinzler, Kenneth W, Vogelstein, Bert, Wissner, Allan, Nunes, Maria, Discafani, Carolyn M

“…A combination of two drugs afforded remarkable protection from intestinal neoplasia in APC(Min/+) mice, a murine model of human familial adenomatous polyposis…”
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Optimization of 6,7-Disubstituted-4-(arylamino)quinoline-3-carbonitriles as Orally Active, Irreversible Inhibitors of Human Epidermal Growth Factor Receptor-2 Kinase Activity by Tsou, Hwei-Ru, Overbeek-Klumpers, Elsebe G, Hallett, William A, Reich, Marvin F, Floyd, M. Brawner, Johnson, Bernard D, Michalak, Ronald S, Nilakantan, Ramaswamy, Discafani, Carolyn, Golas, Jonathan, Rabindran, Sridhar K, Shen, Ru, Shi, Xiaoqing, Wang, Yu-Fen, Upeslacis, Janis, Wissner, Allan

“…A series of new 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitrile derivatives that function as irreversible inhibitors of human epidermal growth factor…”
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Parallel synthesis and biological evaluation of 5,6,7,8-tetrahydrobenzothieno[2,3- d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells by Jennings, Lee D., Kincaid, Scott L., Wang, Yanong D., Krishnamurthy, Girija, Beyer, Carl F., McGinnis, John P., Miranda, Miriam, Discafani, Carolyn M., Rabindran, Sridhar K.

“…A novel series of anti-proliferative agents containing the thieno[2,3- d]pyrimidin-4-one scaffold and the structure–activity relationship studies to improve…”
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Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2) by Wissner, Allan, Overbeek, Elsebe, Reich, Marvin F, Floyd, M. Brawner, Johnson, Bernard D, Mamuya, Nellie, Rosfjord, Edward C, Discafani, Carolyn, Davis, Rachel, Shi, Xiaoqing, Rabindran, Sridhar K, Gruber, Brian C, Ye, Fei, Hallett, William A, Nilakantan, Ramaswamy, Shen, Ru, Wang, Yu-Fen, Greenberger, Lee M, Tsou, Hwei-Ru

“…A series of of 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile derivatives that function as irreversible inhibitors of EGFR and HER-2 kinases have been…”
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HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo by LOGANZO, Frank, DISCAFANI, Carolyn M, SINGANALLORE, Thiruvikraman, KHAFIZOVA, Gulnaz, PORUCHYNSKY, Marianne S, FOJO, Tito, NIEMAN, James A, AYRAL-KALOUSTIAN, Semiramis, ZASK, Arie, ANDERSEN, Raymond J, GREENBERGER, Lee M, ANNABLE, Tami, BEYER, Carl, MUSTO, Sylvia, HARI, Malathi, XINGZHI TAN, HARDY, Carolyn, HERNANDEZ, Richard, BAXTER, Michelle

“…Hemiasterlin is a natural product derived from marine sponges that, like other structurally diverse peptide-like molecules, binds to the Vinca-peptide site in…”
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Synthesis and SAR of 6-chloro-4-fluoroalkylamino-2-heteroaryl-5-(substituted)phenylpyrimidines as anti-cancer agents by Zhang, Nan, Ayral-Kaloustian, Semiramis, Nguyen, Thai, Hernandez, Richard, Lucas, Judy, Discafani, Carolyn, Beyer, Carl

“…The synthesis and SAR of a series of 6-chloro-4-fluoroalkylamino-2-heteroaryl-5-(substituted)phenylpyrimidines as anti-cancer agents are described. This series…”
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MAC-321, a novel taxane with greater efficacy than paclitaxel and docetaxel in vitro and in vivo by Sampath, Deepak, Discafani, Carolyn M, Loganzo, Frank, Beyer, Carl, Liu, Hao, Tan, Xingzhi, Musto, Sylvia, Annable, Tami, Gallagher, Patricia, Rios, Carol, Greenberger, Lee M

“…The taxanes, paclitaxel (PTX) and docetaxel (DTX), belong to a novel class of anticancer drugs that stabilize microtubules and lead to tumor cell death. While…”
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Preclinical Pharmacologic Evaluation of MST-997, an Orally Active Taxane with Superior In vitro and In vivo Efficacy in Paclitaxel- and Docetaxel-Resistant Tumor Models by SAMPATH, Deepak, GREENBERGER, Lee M, BEYER, Carl, HARI, Malathi, HAO LIU, BAXTER, Michelle, YANG, Sharon, RIOS, Carol, DISCAFANI, Carolyn

“…Purpose: Because resistance to paclitaxel and docetaxel is frequently observed in the clinic, new anti-microtubule agents have been sought. The aim of this…”
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Identification of 4-anilino-3-quinolinecarbonitrile inhibitors of mitogen-activated protein/extracellular signal-regulated kinase 1 kinase by Mallon, Robert, Feldberg, Larry, Kim, Steven, Collins, Karen, Wojciechowicz, Donald, Kohler, Constance, Kovacs, Diana, Discafani, Carolyn, Zhang, Nan, Wu, Biqi, Floyd, Brawner, Powell, Dennis, Berger, Dan

“…A high-throughput screen for Ras–mitogen-activated protein kinase (MAPK) signaling inhibitors identified two series (class 1 and 2 ) of substituted…”
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Namenamicin, a New Enediyne Antitumor Antibiotic from the Marine Ascidian Polysyncraton lithostrotum by McDonald, Leonard A, Capson, Todd L, Krishnamurthy, Girija, Ding, Wei-Dong, Ellestad, George A, Bernan, Valerie S, Maiese, William M, Lassota, Piotr, Kramer, Robert A, Ireland, Chris M

“…Marine ascidians belonging to the family Didemnidae have proven a remarkable source of chemically diverse natural products with potent biological properties…”
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Spiroxins, DNA cleaving antitumor antibiotics from a marine-derived fungus by McDonald, Leonard A., Abbanat, Darren R., Barbieri, Laurel R., Bernan, Valerie S., Discafani, Carolyn M., Greenstein, Michael, Janota, Katarzyna, Korshalla, Joseph D., Lassota, Piotr, Tischler, Mark, Carter, Guy T.

“…The spiroxins ( 1–5) were purified from the culture extract of a marine-derived fungus. Their unique bisnaphthospiroketal structures were established by NMR…”
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TTI-237 : A Novel Microtubule-Active Compound with In vivo Antitumor Activity by BEYER, Carl F, NAN ZHANG, HERNANDEZ, Richard, VITALE, Danielle, LUCAS, Judy, NGUYEN, Thai, DISCAFANI, Carolyn, AYRAL-KALOUSTIAN, Semiramis, GIBBONS, James J

“…5-Chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-N-[(1S)-2,2,2-trifluoro-1-methylethyl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine butanedioate…”
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Histopathology of salivary and mammary gland tumors in transgenic mice expressing a human Ha-ras oncogene by NIELSEN, L. L, DISCAFANI, C. M, GURNANI, M, TYLER, R. D

“…Mutated ras genes are powerful transforming agents in vitro and are found in a wide variety of human tumors in vivo. We characterized the histopathology and…”
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SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models by GALAS, Jennifer M, LUCAS, Judy, FANGBIAO LI, TITSCH, Craig, HUSELTON, Christine, CHAUDHARY, Inder, BOSCHELLI, Frank, ETIENNE, Carlo, GOLAS, Jonathan, DISCAFANI, Carolyn, SRIDHARAN, Latha, BOGHAERT, Erwin, ARNDT, Kim, FEI YE, BOSCHELLI, Diane H

“…Src up-regulation is a common event in human cancers. In colorectal cancer, increased Src levels are an indicator of poor prognosis, and progression to…”
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6-Substituted-4-(3-bromophenylamino)quinazolines as Putative Irreversible Inhibitors of the Epidermal Growth Factor Receptor (EGFR) and Human Epidermal Growth Factor Receptor (HER-2) Tyrosine Kinases with Enhanced Antitumor Activity by Tsou, Hwei-Ru, Mamuya, Nellie, Johnson, Bernard D, Reich, Marvin F, Gruber, Brian C, Ye, Fei, Nilakantan, Ramaswamy, Shen, Ru, Discafani, Carolyn, DeBlanc, Ronald, Davis, Rachel, Koehn, Frank E, Greenberger, Lee M, Wang, Yu-Fen, Wissner, Allan

“…A series of new 6-substituted-4-(3-bromophenylamino)quinazoline derivatives that may function as irreversible inhibitors of epidermal growth factor receptor…”
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Synthesis, SAR study and biological evaluation of novel pyrazolo[1,5- a]pyrimidin-7-yl phenyl amides as anti-proliferative agents by Wang, Yanong D., Honores, Erick, Wu, Biqi, Johnson, Steve, Powell, Dennis, Miranda, Miriam, McGinnis, John P., Discafani, Carolyn, Rabindran, Sridhar K., Cheng, Wendy, Krishnamurthy, Girija

“…Checkpoint deficiency of malignant cells can be exploited in cancer drug discovery. Compounds that selectively kill checkpoint-deficient cells versus…”
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Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity by Boschelli, Diane H, Ye, Fei, Wang, Yanong D, Dutia, Minu, Johnson, Steve L, Wu, Biqi, Miller, Karen, Powell, Dennis W, Yaczko, Deanna, Young, Mairead, Tischler, Mark, Arndt, Kim, Discafani, Carolyn, Etienne, Carlo, Gibbons, Jay, Grod, Janet, Lucas, Judy, Weber, Jennifer M, Boschelli, Frank

“…Subsequent to the discovery of 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (1a) as an inhibitor of Src kinase activity (IC50 = 30 nM),…”
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2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as Covalent-Binding, Irreversible Inhibitors of the Kinase Domain of Vascular Endothelial Growth Factor Receptor-2 by Wissner, Allan, Floyd, M. Brawner, Johnson, Bernard D, Fraser, Heidi, Ingalls, Charles, Nittoli, Thomas, Dushin, Russell G, Discafani, Carolyn, Nilakantan, Ramaswamy, Marini, Joseph, Ravi, Malini, Cheung, Kinwang, Tan, Xingzhi, Musto, Sylvia, Annable, Tami, Siegel, Marshall M, Loganzo, Frank

“…A series of 2-(quinazolin-4-ylamino)-[1,4] benzoquinone derivatives that function as potent covalent-binding, irreversible inhibitors of the kinase domain of…”
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