908111-35-3Relevant academic research and scientific papers
COMBINATION THERAPY FOR TREATING CANCER
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, (2019/02/02)
A method of treating cancer comprising administering an effective amount of each of a chemotherapeutic agent and an Hsp90 inhibitor, either separately or as a covalent conjugate of the two, to provide a combination therapy having an enhanced therapeutic e
OMEGA-AMINO ACID DERIVATIVES OF BENZENE, PYRIDINE, AND PYRIDAZINE COMPOUNDS
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, (2015/12/23)
Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1/sub
Design, synthesis, and evaluation of small molecule Hsp90 probes
Taldone, Tony,Zatorska, Danuta,Patel, Pallav D.,Zong, Hongliang,Rodina, Anna,Ahn, James H.,Moulick, Kamalika,Guzman, Monica L.,Chiosis, Gabriela
, p. 2603 - 2614 (2011/06/17)
A number of compounds from different chemical classes are known to bind competitively to the ATP-pocket of Hsp90 and inhibit its chaperone function. The natural product geldanamycin was the first reported inhibitor of Hsp90 and since then synthetic inhibitors from purine, isoxazole and indazol-4-one chemical classes have been discovered and are currently or soon to be in clinical trials for the treatment of cancer. In spite of a similar binding mode to Hsp90, distinct biological profiles were demonstrated among these molecules, both in vitro and in vivo. To better understand the molecular basis for these dissimilarities, we report here the synthesis of chemical tools for three Hsp90 inhibitor classes. These agents will be useful for probing tumor-by-tumor the Hsp90 complexes isolated by specific inhibitors. Such information will lead to better understanding of tumor specific molecular markers to aid in their clinical development. It will also help to elucidate the molecular basis for the biological differences observed among Hsp90 inhibitors.
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents
Huang, Kenneth H.,Veal, James M.,Fadden, R. Patrick,Rice, John W.,Eaves, Jeron,Strachan, Jon-Paul,Barabasz, Amy F.,Foley, Briana E.,Barta, Thomas E.,Ma, Wei,Silinski, Melanie A.,Hu, Mei,Partridge, Jeffrey M.,Scott, Anisa,DuBois, Laura G.,Freed, Tiffany,Steed, Paul M.,Ommen, Andy J.,Smith, Emilie D.,Hughes, Philip F.,Woodward, Angela R.,Hanson, Gunnar J.,McCall, W. Stephen,Markworth, Christopher J.,Hinkley, Lindsay,Jenks, Matthew,Geng, Lifeng,Lewis, Meredith,Otto, James,Pronk, Bert,Verleysen, Katleen,Hall, Steven E.
experimental part, p. 4288 - 4305 (2010/01/16)
A novel class of heat shock protein 90 (Hsp90) inhibitors was developed from an unbiased screen to identify protein targets for a diverse compound library. These indol-4-one and indazol-4-one derived 2-aminobenzamides showed strong binding affinity to Hsp
TETRAHYDROINDOLONE AND TETRAHYDROINDAZOLONE DERIVATIVES
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Page/Page column 102, (2008/06/13)
Disclosed are compounds and pharmaceutically acceptable salts of Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined
