Zobrazeno 1 - 10
of 83
pro vyhledávání: '"Allan Wissner"'
Autor:
Xin Han, Charles Ingalls, Russell Dushin, Middleton Brawner Floyd, Thomas Nittoli, Katherine Cheung, Yongbo Hu, K T Arndt, G. Grosu, Bing Guo, Heidi L. Fraser, Allan Wissner, Andrea Olland
Publikováno v:
European Journal of Medicinal Chemistry. 45:1379-1386
A series of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamine-based inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1) has been identified. Several examples appear to be potent and relatively selective inhibito
Publikováno v:
Journal of Medicinal Chemistry. 52:1493-1509
Autor:
Allan Wissner, Tarek S. Mansour
Publikováno v:
Archiv der Pharmazie. 341:465-477
The development of HKI-272 and EKB-569 for the treatment of cancer is described. These compounds function as irreversible inhibitors of some members of the ErbB family of receptor tyrosine kinases. In particular, they target epidermal growth factor r
Autor:
Frank Loganzo, Charles Ingalls, Thomas Nittoli, Xingzhi Tan, M. Brawner Floyd, Heidi L. Fraser, Kinwang Cheung, Allan Wissner, Russell Dushin, Malini Ravi
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:3635-3648
A series of 4-dimethylamino-but-2-enoic acid [4-(3,6-dioxo-cyclohexa-1,4-dienylamino)-7-ethoxy-quinazolin-6-yl]-amide derivatives were prepared. These compounds have two independent reactive centers and were designed to function as dual irreversible
Autor:
Brian W. Brannigan, Godin-Heymann Nadia G, Kurt J. Isselbacher, Daniel A. Haber, David R. Driscoll, Raffaella Sordella, Kwak Eunice L, Jeffrey Settleman, Thomas J. Lynch, Patricia L. Harris, Ross A. Okimoto, John P. McGinnis, Allan Wissner, Sreenath V. Sharma, Sridhar K. Rabindran, Daphne W. Bell, Panos Fidias
Publikováno v:
Proceedings of the National Academy of Sciences. 102:7665-7670
Non-small cell lung cancers (NSCLCs) with activating mutations in the kinase domain of the epidermal growth factor receptor (EGFR) demonstrate dramatic, but transient, responses to the reversible tyrosine kinase inhibitors gefitinib (Iressa) and erlo
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
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
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
Autor:
Hwei-Ru Tsou, Yu-Fen Wang, Ramaswamy Nilakantan, Lee M. Greenberger, M. Brawner Floyd, Ru Shen, Sridhar K. Rabindran, Allan Wissner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2893-2897
The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth i
Autor:
Dennis Powell, Minu Dutia, Berger Dan Maarten, Frenel Fils Demorin, Jennifer Weber, Yuri Raifeld, Allan Wissner, Frank Boschelli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2989-2992
A series of substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles has been prepared as Src kinase inhibitors. Optimal activity is observed with compounds that have basic amines attached via the para position of the 7-phenyl ring, and a hydrogen ato