Design, synthesis and binding affinities of novel non-peptide mimics of somatostatin/sandostatin(R)

被引：33
作者：
Damour, D
Barreau, M
Blanchard, JC
Burgevin, MC
Doble, A
Herman, F
Pantel, G
JamesSurcouf, E
Vuilhorgne, M
Mignani, S
Poitout, L
LeMerrer, Y
Depezay, JC
机构：
[1] RHONE POULENC RORER SA,CTR RECH VITRY ALFORTVILLE,F-94403 VITRY SUR SEINE,FRANCE
[2] UNIV PARIS 05,CHIM & BIOCHIM PHARMACOL & TOXICOL LAB,CNRS,F-75270 PARIS 06,FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 14期
关键词：
D O I：
10.1016/0960-894X(96)00289-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Based on molecular modelling studies of Sandostatin(R), sugar-based derivatives I-VI were prepared as potential non-peptide mimics of somatostatin/Sandostatin(R). These compounds displaced 3-[I-125]-Tyr(11)-SRIF-14 from the somatostatin receptor on membranes of rat cerebral cortex with IC50 values between 10 and 15 mu M. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码：1667 / 1672
页数：6
相关论文
共 26 条
  • [1] DAMOUR D, Patent No. 9505510
  • [2] DEPEZAY JC, Patent No. 9401921
  • [3] EVIDENCE FOR THE BIOACTIVE CONFORMATION IN A CYCLIC HEXAPEPTIDE ANALOG OF SOMATOSTATIN CONTAINING A CIS-PEPTIDE BOND MIMIC
    ELSEVIERS, M
    VANDERAUWERA, L
    PEPERMANS, H
    TOURWE, D
    VANBINST, G
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1988, 154 (02) : 515 - 521
  • [4] ELST V, 1987, INT J PEPT PROT RES, V29, P318
  • [5] NONPEPTIDAL PEPTIDOMIMETICS WITH A BETA-D-GLUCOSE SCAFFOLDING - A PARTIAL SOMATOSTATIN AGONIST BEARING A CLOSE STRUCTURAL RELATIONSHIP TO A POTENT, SELECTIVE SUBSTANCE-P ANTAGONIST
    HIRSCHMANN, R
    NICOLAOU, KC
    PIETRANICO, S
    SALVINO, J
    LEAHY, EM
    SPRENGELER, PA
    FURST, G
    SMITH, AB
    STRADER, CD
    CASCIERI, MA
    CANDELORE, MR
    DONALDSON, C
    VALE, W
    MAECHLER, L
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1992, 114 (23) : 9217 - 9218
  • [6] DE-NOVO DESIGN AND SYNTHESIS OF SOMATOSTATIN NONPEPTIDE PEPTIDOMIMETICS UTILIZING BETA-D-GLUCOSE AS A NOVEL SCAFFOLDING
    HIRSCHMANN, R
    NICOLAOU, KC
    PIETRANICO, S
    LEAHY, EM
    SALVINO, J
    ARISON, B
    CICHY, MA
    SPOORS, PG
    SHAKESPEARE, WC
    SPRENGELER, PA
    HAMLEY, P
    SMITH, AB
    REISINE, T
    RAYNOR, K
    MAECHLER, L
    DONALDSON, C
    VALE, W
    FREIDINGER, RM
    CASCIERI, MR
    STRADER, CD
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1993, 115 (26) : 12550 - 12568
  • [7] 3-DIMENSIONAL QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS OF SOMATOSTATIN ANALOGS .1. COMPARATIVE MOLECULAR-FIELD ANALYSIS OF GROWTH-HORMONE RELEASE-INHIBITING POTENCIES
    HOCART, SJ
    REDDY, V
    MURPHY, WA
    COY, DH
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (11) : 1974 - 1989
  • [8] CLASSIFICATION AND NOMENCLATURE OF SOMATOSTATIN RECEPTORS
    HOYER, D
    BELL, GI
    BERELOWITZ, M
    EPELBAUM, J
    FENIUK, W
    HUMPHREY, PPA
    OCARROLL, AM
    PATEL, YC
    SCHONBRUNN, A
    TAYLOR, JE
    REISINE, T
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1995, 16 (03) : 86 - 88
  • [9] MAIN CHAIN AND SIDE-CHAIN CHIRAL METHYLATED SOMATOSTATIN ANALOGS - SYNTHESES AND CONFORMATIONAL-ANALYSES
    HUANG, ZW
    HE, YB
    RAYNOR, K
    TALLENT, M
    REISINE, T
    GOODMAN, M
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1992, 114 (24) : 9390 - 9401
  • [10] MINIREVIEW - PHARMACOLOGICAL STUDIES OF SOMATOSTATIN AND SOMATOSTATIN-ANALOGS - THERAPEUTIC ADVANCES AND PERSPECTIVES
    MOREAU, JP
    DEFEUDIS, FV
    [J]. LIFE SCIENCES, 1987, 40 (05) : 419 - 437
123