共 16 条
THE SQUALESTATINS - POTENT INHIBITORS OF SQUALENE SYNTHASE, 3-HYDROXYMETHYL DERIVATIVES
被引:14
作者:

COX, B
论文数: 0 引用数: 0
h-index: 0
机构: Glaxo Research and Development Ltd, Greenford

HUTSON, JL
论文数: 0 引用数: 0
h-index: 0
机构: Glaxo Research and Development Ltd, Greenford

KEELING, SE
论文数: 0 引用数: 0
h-index: 0
机构: Glaxo Research and Development Ltd, Greenford

KIRK, BE
论文数: 0 引用数: 0
h-index: 0
机构: Glaxo Research and Development Ltd, Greenford

SRIKANTHA, ARP
论文数: 0 引用数: 0
h-index: 0
机构: Glaxo Research and Development Ltd, Greenford

WATSON, NS
论文数: 0 引用数: 0
h-index: 0
机构: Glaxo Research and Development Ltd, Greenford
机构:
[1] Glaxo Research and Development Ltd, Greenford
关键词:
D O I:
10.1016/S0960-894X(01)80537-0
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
A series of 3-hydroxymethyl derivatives of squalestatin 1 was prepared as inhibitors of squalene synthase. Potent in vitro inhibitory activity is retained in those analogues which possess C-6 and C-1 substituents analogous to those found in 1.
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页码:1931 / 1936
页数:6
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- [1] ZARAGOZIC ACIDS - A FAMILY OF FUNGAL METABOLITES THAT ARE PICOMOLAR COMPETITIVE INHIBITORS OF SQUALENE SYNTHASE[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (01) : 80 - 84BERGSTROM, JD论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065KURTZ, MM论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065REW, DJ论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065AMEND, AM论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065KARKAS, JD论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065BOSTEDOR, RG论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065BANSAL, VS论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065DUFRESNE, C论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065VANMIDDLESWORTH, FL论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065HENSENS, OD论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065LIESCH, JM论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065ZINK, DL论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065WILSON, KE论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065ONISHI, J论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065MILLIGAN, JA论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065BILLS, G论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065KAPLAN, L论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065OMSTEAD, MN论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065JENKINS, RG论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065HUANG, L论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065MEINZ, MS论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065QUINN, L论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065BURG, RW论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065KONG, YL论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065MOCHALES, S论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065MOJENA, M论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065MARTIN, I论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065PELAEZ, F论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065DIEZ, MT论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065ALBERTS, AW论文数: 0 引用数: 0 h-index: 0机构: MERCK RES LABS,DEPT NAT PROD CHEM,RAHWAY,NJ 07065
- [2] THE SQUALESTATINS - C-3 DECARBOXYLATION STUDIES AND REARRANGEMENT TO THE 6,8-DIOXABICYCLO[3.2.1]OCTANE RING-SYSTEM[J]. TETRAHEDRON LETTERS, 1993, 34 (38) : 6143 - 6146CHAN, C论文数: 0 引用数: 0 h-index: 0机构: Department of Medicinal Chemistry, Glaxo Group Research Ltd., Greenford, Middlesex UB6 0HF, Greenford RoadINGLIS, GGA论文数: 0 引用数: 0 h-index: 0机构: Department of Medicinal Chemistry, Glaxo Group Research Ltd., Greenford, Middlesex UB6 0HF, Greenford RoadPROCOPIOU, PA论文数: 0 引用数: 0 h-index: 0机构: Department of Medicinal Chemistry, Glaxo Group Research Ltd., Greenford, Middlesex UB6 0HF, Greenford RoadROSS, BC论文数: 0 引用数: 0 h-index: 0机构: Department of Medicinal Chemistry, Glaxo Group Research Ltd., Greenford, Middlesex UB6 0HF, Greenford RoadSRIKANTHA, ARP论文数: 0 引用数: 0 h-index: 0机构: Department of Medicinal Chemistry, Glaxo Group Research Ltd., Greenford, Middlesex UB6 0HF, Greenford RoadWATSON, NS论文数: 0 引用数: 0 h-index: 0机构: Department of Medicinal Chemistry, Glaxo Group Research Ltd., Greenford, Middlesex UB6 0HF, Greenford Road
- [3] THE SQUALESTATINS, NOVEL INHIBITORS OF SQUALENE SYNTHASE PRODUCED BY A SPECIES OF PHOMA .1. TAXONOMY, FERMENTATION, ISOLATION, PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL-ACTIVITY[J]. JOURNAL OF ANTIBIOTICS, 1992, 45 (05) : 639 - 647DAWSON, MJ论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDFARTHING, JE论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDMARSHALL, PS论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDMIDDLETON, RF论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDONEILL, MJ论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDSHUTTLEWORTH, A论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDSTYLLI, C论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDTAIT, RM论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDTAYLOR, PM论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDWILDMAN, HG论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDBUSS, AD论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDLANGLEY, D论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLANDHAYES, MV论文数: 0 引用数: 0 h-index: 0机构: GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND GLAXO GRP RES LTD,DEPT BIOCHEM TARGETS,GREENFORD UB6 0HE,MIDDX,ENGLAND
- [4] NOTIZ UBER DIE SELEKTIVITAT DER SPALTUNG VON CARBONSAURE-METHYLESTERN MIT LITHIUMJODID[J]. HELVETICA CHIMICA ACTA, 1960, 43 (01) : 113 - 118ELSINGER, F论文数: 0 引用数: 0 h-index: 0SCHREIBER, J论文数: 0 引用数: 0 h-index: 0ESCHENMOSER, A论文数: 0 引用数: 0 h-index: 0
- [5] SEMISYNTHETIC SQUALESTATINS - SQUALENE SYNTHASE INHIBITION AND ANTIFUNGAL ACTIVITY - THE SAR OF C6 AND C7 MODIFICATIONS[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (12) : 2605 - 2610GIBLIN, GMP论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordBELL, R论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordHANCOCK, AP论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordHARTLEY, CD论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordINGLIS, GGA论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordPAYNE, JJ论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordPROCOPIOU, PA论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordSHINGLER, AH论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordSMITH, C论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, GreenfordSPOONER, SJ论文数: 0 引用数: 0 h-index: 0机构: Departments of Medicinal Chemistry, Glaxo Group Research, Greenford
- [6] THE ZARAGOZIC ACIDS - STRUCTURE ELUCIDATION OF A NEW CLASS OF SQUALENE SYNTHASE INHIBITORS[J]. TETRAHEDRON LETTERS, 1993, 34 (03) : 399 - 402HENSENS, OD论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories, Rahway, NJ 07065-0900DUFRESNE, C论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories, Rahway, NJ 07065-0900LIESCH, JM论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories, Rahway, NJ 07065-0900ZINK, DL论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories, Rahway, NJ 07065-0900REAMER, RA论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories, Rahway, NJ 07065-0900VANMIDDLESWORTH, F论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories, Rahway, NJ 07065-0900
- [7] THE SYNTHESIS OF C3-METHYL, C3-DECARBOXY-ZARAGOZIC ACID-A - A POTENT SQUALENE SYNTHASE INHIBITOR[J]. TETRAHEDRON LETTERS, 1993, 34 (43) : 6863 - 6866KUO, CH论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories P. O., Rahway, NJ 07065PLEVYAK, SP论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories P. O., Rahway, NJ 07065BIFTU, T论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories P. O., Rahway, NJ 07065PARSONS, WH论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories P. O., Rahway, NJ 07065BERGER, GD论文数: 0 引用数: 0 h-index: 0机构: Merck Research Laboratories P. O., Rahway, NJ 07065
- [8] STRUCTURALLY SIMPLIFIED SQUALESTATINS - A CONVENIENT ROUTE TO A 6,7-UNSUBSTITUTED DERIVATIVE[J]. TETRAHEDRON LETTERS, 1993, 34 (27) : 4357 - 4360LESTER, MG论文数: 0 引用数: 0 h-index: 0机构: Glaxo Group Research Ltd, GreenfordGIBLIN, GMP论文数: 0 引用数: 0 h-index: 0机构: Glaxo Group Research Ltd, GreenfordINGLIS, GGA论文数: 0 引用数: 0 h-index: 0机构: Glaxo Group Research Ltd, GreenfordPROCOPIOU, PA论文数: 0 引用数: 0 h-index: 0机构: Glaxo Group Research Ltd, GreenfordROSS, BC论文数: 0 引用数: 0 h-index: 0机构: Glaxo Group Research Ltd, GreenfordWATSON, NS论文数: 0 引用数: 0 h-index: 0机构: Glaxo Group Research Ltd, Greenford
- [9] SELECTIVE HYDRIDE-MEDIATED CONJUGATE REDUCTION OF ALPHA,BETA-UNSATURATED CARBONYL-COMPOUNDS USING [(PH3P)CUH]6[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1988, 110 (01) : 291 - 293MAHONEY, WS论文数: 0 引用数: 0 h-index: 0机构: INDIANA UNIV,DEPT CHEM,BLOOMINGTON,IN 47405 INDIANA UNIV,DEPT CHEM,BLOOMINGTON,IN 47405BRESTENSKY, DM论文数: 0 引用数: 0 h-index: 0机构: INDIANA UNIV,DEPT CHEM,BLOOMINGTON,IN 47405 INDIANA UNIV,DEPT CHEM,BLOOMINGTON,IN 47405STRYKER, JM论文数: 0 引用数: 0 h-index: 0机构: INDIANA UNIV,DEPT CHEM,BLOOMINGTON,IN 47405 INDIANA UNIV,DEPT CHEM,BLOOMINGTON,IN 47405
- [10] REDUCTION OF CARBOXYLIC-ACIDS TO ALCOHOLS THROUGH 1-SUCCINIMIDYL ESTERS WITH NABH4[J]. CHEMISTRY LETTERS, 1979, (08) : 981 - 982NIKAWA, J论文数: 0 引用数: 0 h-index: 0SHIBA, T论文数: 0 引用数: 0 h-index: 0