SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGS AS INHIBITORS OF PROTEIN-KINASE-C

被引：29

作者：

MENDOZA, JS

JAGDMANN, GE

GOSNELL, PA

机构：

[1] Sphinx Pharmaceuticals, a Division of Eli Lilly and Company, Durham, NC 27707

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 19期

关键词：

D O I：

10.1016/0960-894X(95)00382-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of conformationally constrained bicyclic (20-25 and 28) and tricyclic (26 and 27) balanol analogues was prepared and evaluated as inhibitors of protein kinase C (PKC). Of special interest are bicyclic balanol analogues 20 and 24 and the tricyclic analogue 26, which not only retain the nanomolar activity for most PKC isozymes, but also display good selectivity over c-AMP dependent protein kinase (PKA).

引用

页码：2211 / 2216

页数：6

共 50 条

[41] Preparation and biological evaluation of conformationally constrained BACE1 inhibitors
Winneroski, Leonard L.
Schiffler, Matthew A.
Erickson, Jon A.
May, Patrick C.
Monk, Scott A.
Timm, David E.
Audia, James E.
Beck, James P.
Boggs, Leonard N.
Borders, Anthony R.
Boyer, Robert D.
Brier, Richard A.
Hudziak, Kevin J.
Klimkowski, Valentine J.
Losada, Pablo Garcia
Mathes, Brian M.
Stout, Stephanie L.
Watson, Brian M.
Mergott, Dustin J.
BIOORGANIC & MEDICINAL CHEMISTRY, 2015, 23 (13) : 3260 - 3268
[42] STRUCTURAL INVESTIGATION OF PROTEIN-KINASE-C INHIBITORS
BARAK, D
SHIBATA, M
REIN, R
JOURNAL OF MOLECULAR STRUCTURE-THEOCHEM, 1991, 76 : 419 - 429
[43] Synthesis and biological evaluation of bicyclic nucleosides as inhibitors of M-tuberculosis thymidylate kinase
Van Daele, Ineke
Munier-Lehmann, Helene
Hendrickx, Pieter M. S.
Marchal, Gilles
Chavarot, Pierre
Froeyen, Matheus
Qing, Li
Martins, Jose C.
Van Calenbergh, Serge
CHEMMEDCHEM, 2006, 1 (10) : 1081 - 1090
[44] Polyoxygenated cinnamoylcoumarins as conformationally constrained analogs of cytotoxic diarylpentanoids: Synthesis and biological activity
Molaverdi, Fatemeh
Khoobi, Mehdi
Emami, Saeed
Alipour, Masoumeh
Firuzi, Omidreza
Foroumadi, Alireza
Dehghan, Gholamreza
Miri, Ramin
Shaki, Fatemeh
Jafarpour, Farnaz
Shafiee, Abbas
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 68 : 103 - 110
[45] THERAPEUTIC POTENTIAL OF PROTEIN-KINASE-C INHIBITORS
BRADSHAW, D
HILL, CH
NIXON, JS
WILKINSON, SE
AGENTS AND ACTIONS, 1993, 38 (1-2): : 135 - 147
[46] TANNINS AS SELECTIVE INHIBITORS OF PROTEIN-KINASE-C
KASHIWADA, Y
NONAKA, GI
NISHIOKA, I
BALLAS, LM
JIANG, JB
JANZEN, WP
LEE, KH
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, 2 (03) : 239 - 244
[47] Synthesis and biological evaluation of conformationally restricted pregabalin analogs.
Ling, R
Wustrow, DJ
Ekhato, VI
Suman-Chauhan, N
Vartanian, MG
Rubin, RJ
Wise, LD
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2000, 219 : U22 - U23
[48] Synthesis and biological evaluation of dimeric imatinib analogs as potent tyrosine kinase inhibitors
Paige, Mikell A.
Newman, Miki
Kindler, Thomas
Gilliland, D. Gary
Bushweller, John H.
Brown, Milton L.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2006, 231
[49] Biological Evaluation of Simplified Analogs of Protein Kinase C Inhibitor Staurosporine
Rolph, Carly
Pelkey, Erin
Mowery, Patricia
FASEB JOURNAL, 2015, 29
[50] The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors
Kazmierski, Wieslaw M.
Miriyala, Nagaraju
Johnson, David K.
Baskaran, Sam
ACS MEDICINAL CHEMISTRY LETTERS, 2021, 12 (11): : 1649 - 1655

← 1 2 3 4 5 →