HIGHLY WATER-SOLUBLE TAXOL DERIVATIVES - 2'-POLYETHYLENEGLYCOL ESTERS AS POTENTIAL PRODRUGS

被引：69

作者：

GREENWALD, RB

PENDRI, A

BOLIKAL, D

GILBERT, CW

机构：

[1] Enzon Inc., Piscataway

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)80411-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2' and 7-polyethylene glycol esters of taxol were prepared and found to be essentially water soluble. The rates of hydrolysis of these compounds were measured under neutral, acidic and physiological (basic) conditions. The half-lives of O and N substituted 2'-esters are short enough to permit their use as prodrugs.

引用

页码：2465 / 2470

页数：6

共 16 条

[1] SYNTHESIS OF CONGENERS AND PRODRUGS .3. WATER-SOLUBLE PRODRUGS OF TAXOL WITH POTENT ANTITUMOR-ACTIVITY
DEUTSCH, HM
GLINSKI, JA
HERNANDEZ, M
HAUGWITZ, RD
NARAYANAN, VL
SUFFNESS, M
ZALKOW, LH
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (04) : 788 - 792
[2] GEHRHARDT H, 1987, POLYM BULL, V18, P487
[3] GREENWALD RB, UNPUB
[4] Harris J. M., 1992, POLYETHYLENE GLYCOL
[5] COMPARATIVE INVITRO CYTOTOXICITY OF TAXOL AND TAXOTERE AGAINST CISPLATIN-SENSITIVE AND CISPLATIN-RESISTANT HUMAN OVARIAN-CARCINOMA CELL-LINES
KELLAND, LR
ABEL, G
[J]. CANCER CHEMOTHERAPY AND PHARMACOLOGY, 1992, 30 (06) : 444 - 450
[6] LONGNECKER SM, 1987, CANCER TREAT REP, V71, P53
[7] SYNTHESIS AND EVALUATION OF SOME WATER-SOLUBLE PRODRUGS AND DERIVATIVES OF TAXOL WITH ANTITUMOR-ACTIVITY
MATHEW, AE
MEJILLANO, MR
NATH, JP
HIMES, RH
STELLA, VJ
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (01) : 145 - 151
[8] PREPARATION AND BIOLOGICAL-ACTIVITY OF TAXOL ACETATES
MELLADO, W
MAGRI, NF
KINGSTON, DGI
GARCIAARENAS, R
ORR, GA
HORWITZ, SB
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1984, 124 (02) : 329 - 336
[9] DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF PROTAXOLS
NICOLAOU, KC
RIEMER, C
KERR, MA
RIDEOUT, D
WRASIDLO, W
[J]. NATURE, 1993, 364 (6436) : 464 - 466
[10] ROWINSKY EK, 1992, SEMIN ONCOL, V19, P646

← 1 2 →