New synthetic inhibitors of microtubule depolymerization

被引：35

作者：

Klar, U ^{[1
]}

Graf, H ^{[1
]}

Schenk, O ^{[1
]}

Röhr, B ^{[1
]}

Schulz, H ^{[1
]}

机构：

[1] Schering AG, Res Labs, D-13342 Berlin, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(98)00226-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new class of borneol esters that might be considered as biological analogs of paclitaxel regarding their action on microtubules has been found. By structure-activity optimizations, compounds stabilizing microtubules much better than paclitaxel while showing a remarkably reduced cytotoxic activity were obtained. This dissoziation will open completely new therapeutic areas. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1397 / 1402

页数：6

共 21 条

[1]

[Anonymous], ANGEW CHEM

[2]

BOLLAG DM, 1995, CANCER RES, V55, P2325

[3] SOME PRACTICAL CONSIDERATIONS AND APPLICATIONS OF THE NATIONAL-CANCER-INSTITUTE IN-VITRO ANTICANCER DRUG DISCOVERY SCREEN [J].

BOYD, MR ;

PAULI, KD .

DRUG DEVELOPMENT RESEARCH, 1995, 34 (02) :91-109

[4] Total synthesis of baccatin III and taxol [J].

Danishefsky, SJ ;

Masters, JJ ;

Young, WB ;

Link, JT ;

Snyder, LB ;

Magee, TV ;

Jung, DK ;

Isaacs, RCA ;

Bornmann, WG ;

Alaimo, CA ;

Coburn, CA ;

DiGrandi, MJ .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1996, 118 (12) :2843-2859

[5] FIRST TOTAL SYNTHESIS OF TAXOL .1. FUNCTIONALIZATION OF THE B-RING [J].

HOLTON, RA ;

SOMOZA, C ;

KIM, HB ;

LIANG, F ;

BIEDIGER, RJ ;

BOATMAN, PD ;

SHINDO, M ;

SMITH, CC ;

KIM, SC ;

NADIZADEH, H ;

SUZUKI, Y ;

TAO, CL ;

VU, P ;

TANG, SH ;

ZHANG, PS ;

MURTHI, KK ;

GENTILE, LN ;

LIU, JH .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1994, 116 (04) :1597-1598

[6]

Kowalski RJ, 1997, J BIOL CHEM, V272, P2534

[7]

LEE VMY, 1994, NEUROBIOL AGING, V15, pS87

[8] Eleutherobin, a new cytotoxin that mimics paclitaxel (Taxol) by stabilizing microtubules [J].

Lindel, T ;

Jensen, PR ;

Fenical, W ;

Long, BH ;

Casazza, AM ;

Carboni, J ;

Fairchild, CR .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1997, 119 (37) :8744-8745

[9]

Masters J.J., 1995, ANGEW CHEM, V107, P1886, DOI DOI 10.1002/ANGE.19951071617

[10]

MICHAELIS ML, 1998, IN PRESS J NEUROCHEM

← 1 2 3 →