Discovery of a 2,4-Disubstituted Pyrrolo[1,2-f][1,2,4]triazine Inhibitor (BMS-754807) of Insulin-like Growth Factor Receptor (IGF-1R) Kinase in Clinical Development
Wittman, Mark D, Carboni, Joan M, Yang, Zheng, Lee, Francis Y, Antman, Melissa, Attar, Ricardo, Balimane, Praveen, Chang, Chiehying, Chen, Cliff, Discenza, Lorell, Frennesson, David, Gottardis, Marco M, Greer, Ann, Hurlburt, Warren, Johnson, Walter, Langley, David R, Li, Aixin, Li, Jianqing, Liu, Peiying, Mastalerz, Harold, Mathur, Arvind, Menard, Krista, Patel, Karishma, Sack, John, Sang, Xiaopeng, Saulnier, Mark, Smith, Daniel, Stefanski, Kevin, Trainor, George, Velaparthi, Upender, Zhang, Guifen, Zimmermann, Kurt, Vyas, Dolatrai M
Published in Journal of medicinal chemistry (10.12.2009)
Published in Journal of medicinal chemistry (10.12.2009)
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Journal Article
New dual inhibitors of EGFR and HER2 protein tyrosine kinases
Fink, Brian E., Vite, Gregory D., Mastalerz, Harold, Kadow, John F., Kim, Soong-Hoon, Leavitt, Kenneth J., Du, Karen, Crews, Donald, Mitt, Toomas, Wong, Tai W., Hunt, John T., Vyas, Dolatrai M., Tokarski, John S.
Published in Bioorganic & medicinal chemistry letters (01.11.2005)
Published in Bioorganic & medicinal chemistry letters (01.11.2005)
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Journal Article
The discovery of BMS-275183: an orally efficacious novel taxane
Mastalerz, Harold, Cook, Donald, Fairchild, Craig R, Hansel, Steven, Johnson, Walter, Kadow, John F, Long, Byron H, Rose, William C, Tarrant, James, Wu, Mu-Jen, Xue, May Quifen, Zhang, Guifen, Zoeckler, Mary, Vyas, Dolatrai M
Published in Bioorganic & medicinal chemistry (01.10.2003)
Published in Bioorganic & medicinal chemistry (01.10.2003)
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Journal Article
Synthesis and Antitumor Activity of Novel C-7 Paclitaxel Ethers: Discovery of BMS-184476
Altstadt, Thomas J, Fairchild, Craig R, Golik, Jerzy, Johnston, Kathy A, Kadow, John F, Lee, Francis Y, Long, Byron H, Rose, William C, Vyas, Dolatrai M, Wong, Henry, Wu, Mu-Jen, Wittman, Mark D
Published in Journal of medicinal chemistry (20.12.2001)
Published in Journal of medicinal chemistry (20.12.2001)
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Journal Article
Discovery and Preclinical Evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic Acid, (3S)-3-Morpholinylmethyl Ester (BMS-599626), a Selective and Orally Efficacious Inhibitor of Human Epidermal Growth Factor Receptor 1 and 2 Kinases
Gavai, Ashvinikumar V, Fink, Brian E, Fairfax, David J, Martin, Gregory S, Rossiter, Lana M, Holst, Christian L, Kim, Soong-Hoon, Leavitt, Kenneth J, Mastalerz, Harold, Han, Wen-Ching, Norris, Derek, Goyal, Bindu, Swaminathan, Shankar, Patel, Bharat, Mathur, Arvind, Vyas, Dolatrai M, Tokarski, John S, Yu, Chiang, Oppenheimer, Simone, Zhang, Hongjian, Marathe, Punit, Fargnoli, Joseph, Lee, Francis Y, Wong, Tai W, Vite, Gregory D
Published in Journal of medicinal chemistry (12.11.2009)
Published in Journal of medicinal chemistry (12.11.2009)
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Journal Article
Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2- f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase
Sampognaro, Anthony J., Wittman, Mark D., Carboni, Joan M., Chang, Chiehying, Greer, Ann F., Hurlburt, Warren W., Sack, John S., Vyas, Dolatrai M.
Published in Bioorganic & medicinal chemistry letters (01.09.2010)
Published in Bioorganic & medicinal chemistry letters (01.09.2010)
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Journal Article
Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
Mastalerz, Harold, Chang, Ming, Gavai, Ashvinikumar, Johnson, Walter, Langley, David, Lee, Francis Y., Marathe, Punit, Mathur, Arvind, Oppenheimer, Simone, Tarrant, James, Tokarski, John S., Vite, Gregory D., Vyas, Dolatrai M., Wong, Henry, Wong, Tai W., Zhang, Hongjian, Zhang, Guifen
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
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Journal Article
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
Mastalerz, Harold, Chang, Ming, Chen, Ping, Dextraze, Pierre, Fink, Brian E., Gavai, Ashvinikumar, Goyal, Bindu, Han, Wen-Ching, Johnson, Walter, Langley, David, Lee, Francis Y., Marathe, Punit, Mathur, Arvind, Oppenheimer, Simone, Ruediger, Edward, Tarrant, James, Tokarski, John S., Vite, Gregory D., Vyas, Dolatrai M., Wong, Henry, Wong, Tai W., Zhang, Hongjian, Zhang, Guifen
Published in Bioorganic & medicinal chemistry letters (01.04.2007)
Published in Bioorganic & medicinal chemistry letters (01.04.2007)
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Journal Article
Synthesis and structure–activity relationship of imidazo(1,2- a)thieno(3,2- e)pyrazines as IKK-β inhibitors
Belema, Makonen, Bunker, Amy, Nguyen, Van N., Beaulieu, Francis, Ouellet, Carl, Qiu, Yuping, Zhang, Yunhui, Martel, Alain, Burke, James R., McIntyre, Kim W., Pattoli, Mark A., Daloisio, Connie, Gillooly, Kathleen M., Clarke, Wendy J., Brassil, Patrick J., Zusi, F. Chris, Vyas, Dolatrai M.
Published in Bioorganic & medicinal chemistry letters (01.08.2007)
Published in Bioorganic & medicinal chemistry letters (01.08.2007)
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Journal Article
5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
Mastalerz, Harold, Chang, Ming, Chen, Ping, Fink, Brian E., Gavai, Ashvinikumar, Han, Wen-Ching, Johnson, Walter, Langley, David, Lee, Francis Y., Leavitt, Kenneth, Marathe, Punit, Norris, Derek, Oppenheimer, Simone, Sleczka, Bogdan, Tarrant, James, Tokarski, John S., Vite, Gregory D., Vyas, Dolatrai M., Wong, Henry, Wong, Tai W., Zhang, Hongjian, Zhang, Guifen
Published in Bioorganic & medicinal chemistry letters (01.09.2007)
Published in Bioorganic & medicinal chemistry letters (01.09.2007)
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Journal Article
2-Aryl-2,2-difluoroacetamide FKBP12 Ligands: Synthesis and X-ray Structural Studies
Dubowchik, Gene M, Vrudhula, Vivekananda M, Dasgupta, Bireshwar, Ditta, Jonathan, Chen, Ti, Sheriff, Steven, Sipman, Karin, Witmer, Mark, Tredup, Jeffrey, Vyas, Dolatrai M, Verdoorn, Todd A, Bollini, Sagarika, Vinitsky, Alexander
Published in Organic letters (13.12.2001)
Published in Organic letters (13.12.2001)
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Journal Article
Novel 1H -(benzimidazol -2 -yl ) -1H -pyridin -2 -one inhibitors of insulin-like growth factor I (IGF-1R) kinase
WITTMAN, Mark D, BALASUBRAMANIAN, Balu, GOTTARDIS, Marco, CHIEHYING CHANG, JACOBSON, Bruce, SUN, Yax, HANSEL, Steven, ZOECKLER, Mary, VYAS, Dolatrai M, STOFFAN, Karen, VELAPARTHI, Upender, PIEYING LIU, KRISHNANATHAN, Subramaniam, CARBONI, Joan, AIXIN LI, GREER, Ann, ATTAR, Ricardo
Published in Bioorganic & medicinal chemistry letters (15.02.2007)
Published in Bioorganic & medicinal chemistry letters (15.02.2007)
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Journal Article
Discovery of a Fluoroindolo[2,3-a]carbazole Clinical Candidate with Broad Spectrum Antitumor Activity in Preclinical Tumor Models Superior to the Marketed Oncology Drug, CPT-11
Saulnier, Mark G, Balasubramanian, Balu N, Long, Byron H, Frennesson, David B, Ruediger, Edward, Zimmermann, Kurt, Eummer, Jeffrey T, St. Laurent, Denis R, Stoffan, Karen M, Naidu, B. Narasimhulu, Mahler, Mikael, Beaulieu, Francis, Bachand, Carol, Lee, Frank Y, Fairchild, Craig R, Stadnick, Linda K, Rose, William C, Solomon, Carola, Wong, Henry, Martel, Alain, Wright, John J, Kramer, Robert, Langley, David R, Vyas, Dolatrai M
Published in Journal of medicinal chemistry (07.04.2005)
Published in Journal of medicinal chemistry (07.04.2005)
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Journal Article
Sordaricin antifungal agents
Quesnelle, Claude A, Gill, Patrice, Dodier, Marco, St. Laurent, Denis, Serrano-Wu, Michael, Marinier, Anne, Martel, Alain, Mazzucco, Charles E, Stickle, Terry M, Barrett, John F, Vyas, Dolatrai M, Balasubramanian, Balu N
Published in Bioorganic & medicinal chemistry letters (10.02.2003)
Published in Bioorganic & medicinal chemistry letters (10.02.2003)
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Journal Article
Synthesis of a hybrid analog of the esperamicin and dynemicin cores
Mastalerz, Harold, Doyle, Terrence W, Kadow, John F, Vyas, Dolatrai M
Published in Tetrahedron letters (25.11.1996)
Published in Tetrahedron letters (25.11.1996)
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Journal Article
Design and Synthesis of a Fluoroindolocarbazole Series as Selective Topoisomerase I Active Agents. Discovery of Water-Soluble 3,9-Difluoro-12,13-dihydro-13-[6-amino-β- d-glucopyranosyl]-5H,13H-benzo[b]- thienyl[2,3-a]pyrrolo[3,4-c]carbazole- 5,7(6H)-dione (BMS-251873) with Curative Antitumor Activity against Prostate Carcinoma Xenograft Tumor Model
Balasubramanian, Balu N, St. Laurent, Denis R, Saulnier, Mark G, Long, Byron H, Bachand, Carol, Beaulieu, Francis, Clarke, Wendy, Deshpande, Milind, Eummer, Jeffrey, Fairchild, Craig R, Frennesson, David B, Kramer, Robert, Lee, Frank Y, Mahler, Mikael, Martel, Alain, Naidu, B. Narasimhulu, Rose, William C, Russell, John, Ruediger, Edward, Solomon, Carola, Stoffan, Karen M, Wong, Henry, Zimmermann, Kurt, Vyas, Dolatrai M
Published in Journal of medicinal chemistry (25.03.2004)
Published in Journal of medicinal chemistry (25.03.2004)
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Journal Article
Pyrrolotriazine-5-carboxylate ester inhibitors of EGFR and HER2 protein tyrosine kinases and a novel one-pot synthesis of C-4 subsitituted pyrrole-2,3-dicarboxylate diesters
Mastalerz, Harold, Gavai, Ashvinikumar V, Fink, Brian, Struzynski, Charles, Tarrant, James, Vite, Gregory D, Wong, Tai W, Zhang, Guifen, Vyas, Dolatrai M
Published in Canadian journal of chemistry (01.04.2006)
Published in Canadian journal of chemistry (01.04.2006)
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Journal Article
Sordarin Oxazepine Derivatives as Potent Antifungal Agents
Serrano-Wu, Michael H., St. Laurent, Denis R., Chen, Yijun, Huang, Stella, Lam, Kin-Ray, Matson, James A., Mazzucco, Charles E., Stickle, Terry M., Tully, Thomas P., Wong, Henry S., Vyas, Dolatrai M., Balasubramanian, Balu N.
Published in Bioorganic & medicinal chemistry letters (07.10.2002)
Published in Bioorganic & medicinal chemistry letters (07.10.2002)
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Journal Article