Preclinical efficacy of thioxanthone SR271425 against transplanted solid tumors of mouse and human origin.
作者： Thomas H. Corbett , Chiab Panchapor , Lisa Polin , Nancy Lowichik , Susan Pugh
关键词:
摘要: A highly active and broadly thioxanthone has been identified: N-[[1-[[2-(Diethylamino)ethyl]amino]-7-methoxy-9-oxo-9H-thioxanthen-4-yl] methylformamide (SR271425, BCN326862, WIN71425). In preclinical testing against a variety of subcutaneously growing solid tumors, the following %T/C Log10 tumor cell kill (LK) values were obtained: Panc-03 T/C = 0, 5/5 cures; Colon-38 (adv. stage) 3/5 cures, 4.9 LK; Mam-16/C 3.5 Mam-17/0 2.8 Colon-26 1/5 3.2 Colon-51 T/C= 2.7 Panc-02 3.1 B16 Melanoma 13%, 4.0 Squamous Lung-LC12 14%, BG-1 human ovarian 16%, 1.3 WSU-Br1 breast 25%, 0.8 LK. The agent was modestly doxorubicin (Adr)-resistant tumors: Mam-17/Adr =23%, Mam-16/C/Adr 1.0 LK, but retained substantial activity taxol-resistant tumor: Mam-16/C/taxol 3%, 2.4 SR271425 IV implanted leukemias, L1210 6.3 LK AML1498 5.3 equally both by oral routes administration, although requiring approximately 30% higher dose route. Based on its antitumor profile, it may be appropriate to evaluate in clinical trials.
springer.com
sci-hub.se 参考文章(13)
Lisa Polin, Frederick Valeriote, Kathryn White, Chiab Panchapor, Susan Pugh, Juiwanna Knight, Patricia LoRusso, Maha Hussain, Elaine Liversidge, Nancy Peltier, Trimurtulu Golakoti, Gregory Patterson, Richard Moore, Thomas H. Corbett, Treatment of human prostate tumors PC-3 and TSU-PR1 with standard and investigational agents in SCID mice Investigational New Drugs. ,vol. 15, pp. 99- 108 ,(1997) , 10.1023/A:1005856605726
Thomas H. Corbett, Frederick A. Valeriote, Lisa Polin, Chiab Panchapor, Susan Pugh, Kathryn White, Nancy Lowichik, Juiwanna Knight, Marie-Christine Bissery, Antoinette Wozniak, Patricia LoRusso, Laura Biernat, Daniel Polin, Lentawn Knight, Sandra Biggar, Darrell Looney, Lisa Demchik, Julie Jones, Lynne Jones, Scott Blair, Kerry Palmer, Sandra Essenmacher, Loretta Lisow, Ken C. Mattes, Paul F. Cavanaugh, James B. Rake, Laurence Baker, Discovery of Solid Tumor Active Agents Using a Soft-Agar-Colony-Formation Disk-Diffusion-Assay Springer, Boston, MA. pp. 35- 87 ,(1992) , 10.1007/978-1-4615-3492-1_3
Thomas Corbett, Fred Valeriote, Patricia LoRusso, Lisa Polin, Chiab Panchapor, Susan Pugh, Kathryn White, Juiwanna Knight, Lisa Demchik, Julie Jones, Lynne Jones, Loretta Lisow, In Vivo Methods for Screening and Preclinical Testing Anticancer Drug Development Guide. pp. 75- 99 ,(1997) , 10.1007/978-1-4615-8152-9_5
Thomas H. Corbett, Frederick A. Valeriote, Lisa Demchik, Nancy Lowichik, Lisa Polin, Chiab Panchapor, Susan Pugh, Kathryn White, Juiwanna Kushner, James Rake, Mark Wentland, Trimurtulu Golakoti, Carl Hetzel, Junichi Ogino, Gregory Patterson, Richard Moore, Discovery of cryptophycin-1 and BCN-183577: Examples of strategies and problems in the detection of antitumor activity in mice Investigational New Drugs. ,vol. 15, pp. 207- 218 ,(1997) , 10.1023/A:1005875015011
Laura Biernat, Patricia LoRusso, Lester M. Werbel, Antoinette J. Wozniak, Thomas H. Corbett, Wilbur R. Leopold, Lisa Polin, Maria E. Dan, David Capps, Antitumor Efficacy of PD115934 (NSC 366140) against Solid Tumors of Mice Cancer Research. ,vol. 50, pp. 4900- 4905 ,(1990)
K Paull, S E Bates, M Alvarez, A Monks, C Hose, J S Lee, M Grever, A T Fojo, RHODAMINE EFFLUX PATTERNS PREDICT P-GLYCOPROTEIN SUBSTRATES IN THE NATIONAL CANCER INSTITUTE DRUG SCREEN Molecular Pharmacology. ,vol. 46, pp. 627- 638 ,(1994)
Jerome P. Horwitz, Irina Massova, Thomas E. Wiese, Brent H. Besler, Thomas H. Corbett, Comparative molecular field analysis of the antitumor activity of 9H-thioxanthen-9-one derivatives against pancreatic ductal carcinoma 03. Journal of Medicinal Chemistry. ,vol. 37, pp. 781- 786 ,(1994) , 10.1021/JM00032A010
Mark P. Wentland, Robert B. Perni, Ronald G. Powles, Allan G. Hlavac, Kenneth C. Mattes, Thomas H. Corbett, Susan A. Couhglin, James B. Rake, Anti-solid tumor efficacy and preparation of N-[[1-[[2-(diethylamino)ethyl]amino]-9-oxo-9H-thioxanthen-4-yl]methyl]methanesulfonamide (win 33377) and related derivatives☆ Bioorganic & Medicinal Chemistry Letters. ,vol. 4, pp. 609- 614 ,(1994) , 10.1016/S0960-894X(01)80164-5
Thomas Corbett, Nancy Lowichik, Susan Pugh, Lisa Polin, Chiab Panchapor, Kathryn White, Jui-Wanna Knight, Lisa Demchik, Julie Jones, Lynne Jones, Laura Biernat, Patricia Lorusso, Brenda Foster, Lance Heilbrun, James Rake, Kenneth C Mattes, Robert Perni, Ronald G Powles, Allan G Hlavac, Mark P Wentland, Susan A Coughlin, Laurence Baker, Fred Valeriote, Antitumour activity of N-[[1-[[2-(diethylamino)ethyl]amino]-9-oxo-9H-thioxanthen-4-yl]methyl]methanesulfonamide (WIN33377) and analogues Expert Opinion on Investigational Drugs. ,vol. 3, pp. 1281- 1292 ,(1994) , 10.1517/13543784.3.12.1281
Thomas Corbett, Fred Valeriote, Patricia Lorusso, Lisa Polin, Chiab Panchapor, Susan Pugh, Kathryn White, Juiwanna Knight, Lisa Demchik, Julie Jones, Lynne Jones, Nancy Lowichik, Laura Biernat, Brenda Foster, Antoinette Wozniak, Loretta Lisow, Manuel Valdivieso, Larry Baker, Wilbur Leopold, Judith Sebolt, Marie-Christine Bissery, Ken Mattes, Janet Dzubow, James Rake, Robert Perni, Mark Wentland, Susan Coughlin, J. Michael Shaw, Gary Liversidge, Elaine Liversidge, Joseph Bruno, Pramod Sarpotdar, Richard Moore, Gregory Patterson, Tumor Models and the Discovery and Secondary Evaluation of Solid Tumor Active Agents Pharmaceutical Biology. ,vol. 33, pp. 102- 122 ,(1995) , 10.3109/13880209509067092