Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Carolyn Discafani"'
Autor:
James J. Gibbons, Semiramis Ayral-Kaloustian, Carolyn Discafani, Thai Nguyen, Judy Lucas, Danielle Vitale, Richard Hernandez, Nan Zhang, Carl F. Beyer
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 (TTI-237) is a microtubule-active compound of novel structure and function. Structurally, it is one
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16ac1bf6199fe9d451e181b4e511fa7d
https://doi.org/10.1158/0008-5472.c.6496545
https://doi.org/10.1158/0008-5472.c.6496545
Autor:
James J. Gibbons, Semiramis Ayral-Kaloustian, Carolyn Discafani, Thai Nguyen, Judy Lucas, Danielle Vitale, Richard Hernandez, Nan Zhang, Carl F. Beyer
Supplementary Tables 1-5, Figures 1-5 from TTI-237: A Novel Microtubule-Active Compound with In vivo Antitumor Activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8562d9a70a4a1073a7bca6f5db05c361
https://doi.org/10.1158/0008-5472.22370826.v1
https://doi.org/10.1158/0008-5472.22370826.v1
Autor:
Carolyn Discafani, Huili Xia, Elizabeth A. Maher, Yangping Sun, Roman K. Thomas, Yuki Yuza, Matthew Meyerson, James W. Horner, Karen A. Glatt, Sridhar K. Rabindran, Hidefumi Sasaki, Boonim L. Jung, Xiaojun Zhao, Hongbin Ji, Kate McNamara, Michael J. Eck, Albert Mitchell, Roderick T. Bronson, Geoffrey I. Shapiro, Takeshi Shimamura, Alexei Protopopov, Ruqayyah Al-Hashem, Kwok-Kin Wong, Danan Li
Publikováno v:
Proceedings of the National Academy of Sciences. 103:7817-7822
The tyrosine kinase inhibitors gefitinib (Iressa) and erlotinib (Tarceva) have shown anti-tumor activity in the treatment of non-small cell lung cancer (NSCLC). Dramatic and durable responses have occurred in NSCLC tumors with mutations in the tyrosi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b01493e6795a14bf7edf823480c1f757
https://doi.org/10.1073/pnas.0510284103
https://doi.org/10.1073/pnas.0510284103
Autor:
Latha Sridharan, Judy Lucas, Carlo Etienne, Craig Titsch, Inder Chaudhary, Christine Huselton, Diane H. Boschelli, Jennifer M. Golas, Carolyn Discafani, Erwin R. Boghaert, Frank Boschelli, K T Arndt, Jonathan Golas, Fei Ye, Fangbiao Li
Publikováno v:
Cancer Research. 65:5358-5364
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 metastatic disease is associated with substantial increases in Src activity. Therefore, we examine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8dbf321e875be4b51a22f7f06ec9d92
https://doi.org/10.1158/0008-5472.can-04-2484
https://doi.org/10.1158/0008-5472.can-04-2484
Autor:
Sylvia Musto, Arie Zask, Chuan Niu, Carolyn Discafani, Frank Loganzo, Tami Annable, Richard Hernandez, Emily B. Norton, Semiramis Ayral-Kaloustian, Carl Beyer, Ayako Yamashita, Joshua Kaplan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:5317-5322
Analogs of hemiasterlin (1) and HTI-286 (2), which contain various aromatic rings in the A segment, were synthesized as potential inhibitors of tubulin polymerization. The structure-activity relationships related to stereo- and regio-chemical effects
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9e072e5089cfbeaa24d18c142014b58
https://doi.org/10.1016/j.bmcl.2004.08.024
https://doi.org/10.1016/j.bmcl.2004.08.024
Autor:
Richard Hernandez, Girija Krishnamurthy, Frank Loganzo, Arie Zask, Ayako Yamashita, Gary Harold Birnberg, Lee M. Greenberger, Zhilian Tang, Sylvia Musto, Tami Annable, Derek C. Cole, Xiaoran Yang, Robert Williamson, Semiramis Ayral-Kaloustian, Gulnaz Khafizova, Carolyn Discafani, Emily B. Norton, Katherine Cheung, Chuan Niu, Ronald Suayan, Joshua Kaplan, Carl Beyer
Publikováno v:
Journal of Medicinal Chemistry. 47:4774-4786
Hemiasterlin (1), a tripeptide isolated from marine sponges, induces microtubule depolymerization and mitotic arrest in cells. HTI-286 (2), an analogue from an initial study of the hemiasterlins, is presently in clinical trials. In addition to its po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8b0b9a3feebc73807dca433c28936000
https://doi.org/10.1021/jm040056u
https://doi.org/10.1021/jm040056u
Antitumor Activity of HKI-272, an Orally Active, Irreversible Inhibitor of the HER-2 Tyrosine Kinase
Autor:
Xiaoqing Shi, Bernard Dean Johnson, Carolyn Discafani, Ramaswamy Nilakantan, Edward Rosfjord, Hwei-Ru Tsou, Michelle Baxter, Allan Wissner, Ru Shen, W. A. Hallett, Marvin F Reich, M. Brawner Floyd, Elsebe Overbeek, Sridhar K. Rabindran, Yu-Fen Wang, Jonathan Golas
Publikováno v:
Cancer Research. 64:3958-3965
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 breast cancer patients and predicts a poor outcome in patients with primary disease. Tras
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd04b2d6d2ab228cad72dfb5623aa655
https://doi.org/10.1158/0008-5472.can-03-2868
https://doi.org/10.1158/0008-5472.can-03-2868
Autor:
Karen Collins, Nan Zhang, Robert Mallon, Steven C. Kim, Allan Wissner, Carolyn Discafani, Dennis Powell, Constance Kohler, Jeremy I. Levin, Donald Wojciechowicz, Diane H. Boschelli, Dan Maarten Berger, Minu Dutia, Xuemei Du, Nancy Torres, Larry Feldberg, Biqi Wu, M. Brawner Floyd
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3031-3034
4-[3-Chloro-4-(1-methyl-1H-imidazol-2-ylsulfanyl)]anilino-6,7-diethoxy-3-quinolinecarbonitrile (3) was identified as a MEK1 kinase inhibitor with exceptional activity against LoVo cells. The structure-activity relationships of the C-4 aniline substit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7348c798cec640b4049d2f270b74eb6d
https://doi.org/10.1016/s0960-894x(03)00640-1
https://doi.org/10.1016/s0960-894x(03)00640-1
Autor:
Chris Ireland, William Aalbersberg, Raymond Andersen, Semiramis Ayral-Kaloustian, Roberto Berlinck, Valerie Bernan, Guy Carter, Alice Churchill, Jon Clardy, Gisela Concepcion, E. De Silva, Carolyn Discafani, Tito Fojo, Philip Frost, Donna Gibson, Lee Greenberger, Michael Greenstein, Mary Kay Harper, Robert Mallon, Frank Loganzo, Maria Nunes, Marianne Poruchynsky, Arie Zask
Publikováno v:
Pharmaceutical Biology. 41:15-38
The National Cooperative Natural Products Drug Discovery Group (NCNPDDG) “Anticancer Agents from Unique Natural Products Sources, CA 67786” was first awarded in September 1995. The goal of the project is to discover and develop novel anticancer a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::717069cef7d6e5561faf7d88ddd43f77
https://doi.org/10.1080/1388020039051742
https://doi.org/10.1080/1388020039051742
Autor:
Carolyn Discafani, Bernard Dean Johnson, Hwei-Ru Tsou, Edward Rosfjord, Lee M. Greenberger, M. Brawner Floyd, Rachel Davis, Ramaswamy Nilakantan, Fei Ye, W. A. Hallett, Ru Shen, Allan Wissner, Sridhar K. Rabindran, Brian C. Gruber, Marvin F Reich, Elsebe Overbeek, Yu-Fen Wang, Nellie Mamuya, Xiaoqing Shi
Publikováno v:
Journal of Medicinal Chemistry. 46:49-63
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 prepared. These inhibitors have, at the 6-position, butynamide, crotonamide, and methacrylamid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9e2c5aac82399cca763ede3215dbabf
https://doi.org/10.1021/jm020241c
https://doi.org/10.1021/jm020241c