4-DEACETYLTAXOL AND 10-ACETYL-4-DEACETYLTAXOTERE - SYNTHESIS AND BIOLOGICAL EVALUATION

被引：25

作者：

DATTA, A ^{[1
]}

JAYASINGHE, LR ^{[1
]}

GEORG, GI ^{[1
]}

机构：

[1] OREAD LABS INC,LAWRENCE,KS 66047

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 24期

关键词：

D O I：

10.1021/jm00050a023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-Deacetyltaxol and 10-acetyl-4-deacetyltaxotere were synthesized for the first time from 7-(triethylsilyl)-4-deacetylbaccatin III. These analogs were found to be inactive in the microtubule assembly assay.

引用

页码：4258 / 4260

页数：3

共 19 条

[1]

BOGE TC, IN PRESS J MED CHEM

[2] SYNTHESIS OF 10-DEACETOXYTAXOL AND 10-DEOXYTAXOTERE [J].

CHAUDHARY, AG ;

KINGSTON, DGI .

TETRAHEDRON LETTERS, 1993, 34 (31) :4921-4924

[3] TAXOL STRUCTURE-ACTIVITY-RELATIONSHIPS - SYNTHESIS AND BIOLOGICAL EVALUATION OF 2-DEOXYTAXOL [J].

CHEN, SH ;

WEI, JM ;

FARINA, V .

TETRAHEDRON LETTERS, 1993, 34 (20) :3205-3206

[4] SYNTHESIS OF 7-DEOXYTAXOL AND 7,10-DIDEOXYTAXOL VIA RADICAL INTERMEDIATES [J].

CHEN, SH ;

HUANG, S ;

KANT, J ;

FAIRCHILD, C ;

WEI, JM ;

FARINA, V .

JOURNAL OF ORGANIC CHEMISTRY, 1993, 58 (19) :5028-5029

[5] IMPROVED PROTECTION AND ESTERIFICATION OF A PRECURSOR OF THE TAXOTERE(R) AND TAXOL SIDE-CHAINS [J].

COMMERCON, A ;

BEZARD, D ;

BERNARD, F ;

BOURZAT, JD .

TETRAHEDRON LETTERS, 1992, 33 (36) :5185-5188

[6] INTERNAL NUCLEOPHILE ASSISTED SELECTIVE DEESTERIFICATION STUDIES ON BACCATIN-III - SYNTHESIS OF 2-DEBENZOYLBACCATIN-III AND 4-DEACETYLBACCATIN-III ANALOGS [J].

DATTA, A ;

JAYASINGHE, LR ;

GEORG, GI .

JOURNAL OF ORGANIC CHEMISTRY, 1994, 59 (16) :4689-4690

[7] SYNTHESIS OF BIOLOGICALLY-ACTIVE TAXOL ANALOGS WITH MODIFIED PHENYLISOSERINE SIDE-CHAINS [J].

GEORG, GI ;

CHERUVALLATH, ZS ;

HIMES, RH ;

MEJILLANO, MR ;

BURKE, CT .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (22) :4230-4237

[8] SAMARIUM DIIODIDE-MEDIATED DEOXYGENATION OF TAXOL - A ONE-STEP SYNTHESIS OF 10-DEACETOXYTAXOL [J].

GEORG, GI ;

CHERUVALLATH, ZS .

JOURNAL OF ORGANIC CHEMISTRY, 1994, 59 (14) :4015-4018

[9]

GEORG GI, 1994, EXPERT OPIN THER PAT, V4, P109

[10]

GEORG GI, 1994, IN PRESS TAXOL SCI A

← 1 2 →