Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 18, 2003, Pages 3091-3095

  Myers, Michael R ^a,b   He, Wei ^a   Hanney, Barbara ^a   Setzer, Natalie ^a   Maguire, Martin P ^a   Zulli, Allison ^a   Bilder, Glenda ^a   Galzcinski, Helen ^a   Amin, Dilip ^a   Needle, Saul ^a   Spada, Alfred P ^a  

^a SANOFI   (France)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACID; PHENYL GROUP; PLATELET DERIVED GROWTH FACTOR RECEPTOR; PLATELET DERIVED GROWTH FACTOR RECEPTOR INHIBITOR; PROTEIN TYROSINE KINASE; QUINOXALINE DERIVATIVE; RECEPTOR BLOCKING AGENT; RPR 101511; UNCLASSIFIED DRUG;

AUTOPHOSPHORYLATION; CONFERENCE PAPER; ENZYME ACTIVITY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; STEREOISOMERISM; STRUCTURE ACTIVITY RELATION;

EID: 12444327192     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00654-1     Document Type: Conference Paper

References (16)

1. (a) He, W.; Myers, M. R.; Spada, A. P.; Hanney, B.; Setzer, N. Abstracts of Papers, 217th ACS National Meeting, Anaheim, CA, March 21-25, 1999; ORGN-30.
2. (b) He, W.; Myers, M. R.; Spada, A. P.; Hanney, B.; Setzer, N.; Maguire, M.; Mailliet, P.; Gontier, S.; Guegen, J.-C.; Cans, P.; Orton, E.; Cheve, M.; Kubiak, G. G.; Shah, H. C.; O'Brien, M. K. Abstracts of Papers, 219th ACS National Meeting, San Francisco, CA, March 26-30, 2000; ORGN-225.
3. (c) He, W.; Myers, M. R.; Spada, A. P.; Hanney, B.; Setzer, N.; Mailliet, P.; Gontier, S.; Guegen, J.-C.; Cans, P.; Orton, E.; Cheve, M.; Kubiak, G. G.; Shah, H. C.; O'Brien, M. K.; Bilder, G. E.; Allen, E.; Bissery, M.-C.; Page, K. ; Natarajan, C.; Jayyosi, Z.; Kelley, M. F.; Toutain, H.; Constan, A.; Amin, D. ; Needle, S.; Galczenski, H.; Wang, W.; Perrone, M. H. Abstracts of Papers, 219th ACS National Meeting, San Francisco, CA, March 26-30, 2000; MEDI-307.
4. (d) Myers, M. R. The SCI-Fine Chemicals sponsored conference Protein Tyrosine Kinases, Good Targets for New Drugs?, London, May 22, 2001.
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7. For a few recent reports of PDGF-R inhibitors see: (a) Matsuno, K.; Nakajima, T.; Ichimura, M.; Giese, N. A.; Yu, J.-C.; Lokker, N. A.; Ushiki, J.; Ide, S.; Oda, S.; Nomoto, Y. J. Med. Chem. 2002, 45, 4513. (b) Mahboobi, S.; Teller, S.; Pongratz, H.; Hufsky, H.; Sellmer, A.; Botzki, A.; Uecker, A.; Beckers, T.; Baasner.; S.; Schaechtele, C.; Ueberall, F.; Kassack, M.U.; Dove, S.; Boehmer, F.-D. J. Med. Chem. 2002, 45, 1002.
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