The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity

被引：24

作者：

Fritzen, EL ^{[1
]}

Brightwell, AS

Erickson, LA

Romero, DL

机构：

[1] Pharmacia & Upjohn Co, Med Chem Res, Kalamazoo, MI 49001 USA

[2] Pharmacia & Upjohn Co, Cell & Mol Biol Res, Kalamazoo, MI 49001 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(00)00069-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A solid phase synthesis of substituted tetrahydroisoquinolines was developed and used to prepare directed libraries of compounds for screening against the protein phosphatase, CDC25B. From these libraries, a compound was found having approximately a 4-fold improvement in activity. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：649 / 652

页数：4

共 17 条

[1] ANCHORING OF FMOC AMINO-ACID TO 4-ALKOXYBENZYL ALCOHOL RESIN USING A NEW ESTERIFICATION REAGENT [J].

AKAJI, K ;

KURIYAMA, N ;

KIMURA, T ;

FUJIWARA, Y ;

KISO, Y .

TETRAHEDRON LETTERS, 1992, 33 (22) :3177-3180

[2] Activation method to prepare a highly reactive acylsulfonamide ''safety-catch'' linker for solid-phase synthesis [J].

Backes, BJ ;

Virgilio, AA ;

Ellman, JA .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (12) :3055-3056

[3] Generation of an UGI library of phosphate mimic-containing compounds and identification of novel dual specific phosphatase inhibitors [J].

Bergnes, G ;

Gilliam, CL ;

Boisclair, MD ;

Blanchard, JL ;

Blake, KV ;

Epstein, DM ;

Pal, K .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (19) :2849-2854

[4] Synthesis and phosphatase inhibitory activity of analogs of sulfircin [J].

Cebula, RE ;

Blanchard, JL ;

Boisclair, MD ;

Pal, K ;

Bockovich, NJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1997, 7 (15) :2015-2020

[5] PYBOP - A NEW PEPTIDE COUPLING REAGENT DEVOID OF TOXIC BY-PRODUCT [J].

COSTE, J ;

LENGUYEN, D ;

CASTRO, B .

TETRAHEDRON LETTERS, 1990, 31 (02) :205-208

[6] Cdc25 protein phosphatases in cell proliferation [J].

Draetta, G ;

Eckstein, J .

BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER, 1997, 1332 (02) :M53-M63

[7] Organic chemistry on solid supports [J].

Fruchtel, JS ;

Jung, G .

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH, 1996, 35 (01) :17-42

[8] Cdc25 cell-cycle phosphatase as a target of c-myc [J].

Galaktionov, K ;

Chen, XC ;

Beach, D .

NATURE, 1996, 382 (6591) :511-517

[9] APPLICATIONS OF COMBINATORIAL TECHNOLOGIES TO DRUG DISCOVERY .1. BACKGROUND AND PEPTIDE COMBINATORIAL LIBRARIES [J].

GALLOP, MA ;

BARRETT, RW ;

DOWER, WJ ;

FODOR, SPA ;

GORDON, EM .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (09) :1233-1251

[10] APPLICATIONS OF COMBINATORIAL TECHNOLOGIES TO DRUG DISCOVERY .2. COMBINATORIAL ORGANIC-SYNTHESIS, LIBRARY SCREENING STRATEGIES, AND FUTURE-DIRECTIONS [J].

GORDON, EM ;

BARRETT, RW ;

DOWER, WJ ;

FODOR, SPA ;

GALLOP, MA .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (10) :1385-1401

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