The squalestatins: Decarboxy and 4-deoxy analogues as potent squalene synthase inhibitors

Journal of Medicinal Chemistry

Volumn 39, Issue 1, 1996, Pages 207-216

  Chan, Chuen ^a   Andreotti, Daniele ^a   Cox, Brian ^a   Dymock, Brian W ^a   Hutson, Julie L ^a   Keeling, Suzanne E ^a   McCarthy, Alun D ^a   Procopiou, Panayiotis A ^a   Ross, Barry C ^a   Sareen, Meenu ^a   Scicinski, Jan J ^a   Sharratt, Peter J ^a   Snowden, Michael A ^a   Watson, Nigel S ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG ANALOG; SQUALENE SYNTHASE INHIBITOR; SQUALESTATIN;

ARTICLE; DRUG DEVELOPMENT; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; INTRAVENOUS DRUG ADMINISTRATION; MARMOSET; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTICHOLESTEREMIC AGENTS; BICYCLO COMPOUNDS, HETEROCYCLIC; CALLITHRIX; CHOLESTEROL; ENZYME INHIBITORS; FARNESYL-DIPHOSPHATE FARNESYLTRANSFERASE; MICROSOMES, LIVER; MOLECULAR STRUCTURE; RATS; SQUALENE; STRUCTURE-ACTIVITY RELATIONSHIP; TRICARBOXYLIC ACIDS;

EID: 13344279394     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9504969     Document Type: Article

References (35)

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15. Subsequent to our publications, Merck also reported on the isolation of zaragozic acids in which zaragozic acid A has the same structure as S1 1. (a) Bergstrom, J. D.; Kurtz, M. M.; Rew, D. J.; Amend, A. M.; Karkas, J. D.; Bostedor, R. G.; Bansal, V. S.; Dufresne, C.; VanMiddlesworth, F. L.; Hensens, O. D.; Liesch, J. M.; Zink, D. L.; Wilson, K. E.; Onishi, J.; Milligan, J. A.; Bills, G.; Kaplan, L.; Nallin Omstead, M.; Jenkins, R. G.; Huang, L.; Meinz, M. S.; Quinn, L.; Burg, R. W.; Kong, Y. L.; Mochales, S.; Mojena, M.; Martin, I.; Pelaez F.; Diez, M. T.; Alberts, A. W. Zaragozic Acids: A Family of Fungal Metabolites that are Picomolar Competitive Inhibitors of Squalene Synthase. Proc. Natl Acad. Sci. U.S.A. 1993, 90, 80-84. (b) Hensens, O. D.; Dufresne, C.; Liesch, J. M.; Zink, D. L.; Reamer, R. A.; Van-Middlesworth, F. The Zaragozic Acids: Structure Elucidation of a New Class of Squalene Synthase Inhibitors. Tetrahedron Lett. 1993, 34, 399-402.
16. Subsequent to our publications, Merck also reported on the isolation of zaragozic acids in which zaragozic acid A has the same structure as S1 1. (a) Bergstrom, J. D.; Kurtz, M. M.; Rew, D. J.; Amend, A. M.; Karkas, J. D.; Bostedor, R. G.; Bansal, V. S.; Dufresne, C.; VanMiddlesworth, F. L.; Hensens, O. D.; Liesch, J. M.; Zink, D. L.; Wilson, K. E.; Onishi, J.; Milligan, J. A.; Bills, G.; Kaplan, L.; Nallin Omstead, M.; Jenkins, R. G.; Huang, L.; Meinz, M. S.; Quinn, L.; Burg, R. W.; Kong, Y. L.; Mochales, S.; Mojena, M.; Martin, I.; Pelaez F.; Diez, M. T.; Alberts, A. W. Zaragozic Acids: A Family of Fungal Metabolites that are Picomolar Competitive Inhibitors of Squalene Synthase. Proc. Natl Acad. Sci. U.S.A. 1993, 90, 80-84. (b) Hensens, O. D.; Dufresne, C.; Liesch, J. M.; Zink, D. L.; Reamer, R. A.; Van-Middlesworth, F. The Zaragozic Acids: Structure Elucidation of a New Class of Squalene Synthase Inhibitors. Tetrahedron Lett. 1993, 34, 399-402.
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35. Unpublished results from these laboratories.