NOVEL A-RING MODIFIED CAMPTOTHECINS AS TOPOISOMERASE-I INHIBITORS

被引：25

作者：

PEEL, MR ^{[1
]}

MILSTEAD, MW ^{[1
]}

STERNBACH, DD ^{[1
]}

BESTERMAN, JM ^{[1
]}

LEITNER, P ^{[1
]}

MORTON, B ^{[1
]}

WALL, ME ^{[1
]}

WANI, MC ^{[1
]}

机构：

[1] RES TRIANGLE INST,RES TRIANGLE PK,NC 27709

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 18期

关键词：

D O I：

10.1016/0960-894X(95)00360-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A camptothecin derivative has been prepared wherein the A-ring is fused to an oxazole ring. The compound was prepared via a Friedlander condensation involving benzoxazole 8 and tricyclic ketone 9. This derivative displays potent topoisomerase I inhibition (IC50 150 nM) when assayed in the 'cleavable complex' assay.

引用

页码：2129 / 2132

页数：4

共 14 条

[1] CHARACTERIZATION OF A MAMMALIAN MUTANT WITH A CAMPTOTHECIN-RESISTANT DNA TOPOISOMERASE-I [J].

ANDOH, T ;

ISHII, K ;

SUZUKI, Y ;

IKEGAMI, Y ;

KUSUNOKI, Y ;

TAKEMOTO, Y ;

OKADA, K .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (16) :5565-5569

[2] PHASE-I AND PHARMACOKINETIC STUDIES OF TOPOTECAN ADMINISTERED AS A 72 OR 120-H CONTINUOUS-INFUSION [J].

BURRIS, HA ;

AWADA, A ;

KUHN, JG ;

ECKARDT, JR ;

COBB, PW ;

RINALDI, DA ;

FIELDS, S ;

SMITH, L ;

VONHOFF, DD .

ANTI-CANCER DRUGS, 1994, 5 (04) :394-402

[3]

ENG WK, 1988, MOL PHARMACOL, V34, P755

[4]

FITTON P, 1982, COMPREHENSIVE ORGANO, V8, P861

[5]

GUPTA RS, 1988, CANCER RES, V48, P6404

[6]

HSIANG YH, 1985, J BIOL CHEM, V260, P4873

[7] SYNTHESIS OF WATER-SOLUBLE (AMINOALKYL)CAMPTOTHECIN ANALOGS - INHIBITION OF TOPOISOMERASE-I AND ANTITUMOR-ACTIVITY [J].

KINGSBURY, WD ;

BOEHM, JC ;

JAKAS, DR ;

HOLDEN, KG ;

HECHT, SM ;

GALLAGHER, G ;

CARANFA, MJ ;

MCCABE, FL ;

FAUCETTE, LF ;

JOHNSON, RK ;

HERTZBERG, RP .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (01) :98-107

[8] SYNTHESIS AND ANTITUMOR-ACTIVITY OF NOVEL WATER-SOLUBLE DERIVATIVES OF CAMPTOTHECIN AS SPECIFIC INHIBITORS OF TOPOISOMERASE-I [J].

LUZZIO, MJ ;

BESTERMAN, JM ;

EMERSON, DL ;

EVANS, MG ;

LACKEY, K ;

LEITNER, PL ;

MCINTYRE, G ;

MORTON, B ;

MYERS, PL ;

PEEL, M ;

SISCO, JM ;

STERNBACH, DD ;

TONG, WQ ;

TRUESDALE, A ;

UEHLING, DE ;

VUONG, A ;

YATES, J .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (03) :395-401

[9]

SAWADA S, 1991, CHEM PHARM BULL, V39, P1446

[10]

WAL ME, 1991, DNA TOPOISOMERASES C, P93

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