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

[11] PLANT ANTITUMOR AGENTS .I. ISOLATION AND STRUCTURE OF CAMPTOTHECIN A NOVEL ALKALOIDAL LEUKEMIA AND TUMOR INHIBITOR FROM CAMPTOTHECA ACUMINATA [J].