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新型细胞毒性苯并(b)噻吩磺酰胺1,1 -二氧化物衍生物可抑制位于肿瘤细胞质膜上的NADH氧化酶。

New cytotoxic benzo(b)thiophenilsulfonamide 1,1-dioxide derivatives inhibit a NADH oxidase located in plasma membranes of tumour cells.

作者信息

Alonso M M, Encío I, Martínez-Merino V, Gil M, Migliaccio M

机构信息

Department of Health Sciences, Public University of Navarra, Avd Barañaín s/n, Pamplona, 31008, Spain.

出版信息

Br J Cancer. 2001 Nov 2;85(9):1400-2. doi: 10.1054/bjoc.2001.2083.

Abstract

A series of benzo(b)thiophenesulfonamide 1,1-dioxide derivatives (BTS) have been designed and synthesized as candidate antineoplastic drugs. Several of these compounds have shown in vitro cytotoxic activity on leukaemic CCRF-CEM cells. The cytotoxic BTS, but not the inactive ones, were able to inhibit a tumour cell-specific NADH oxidase activity present in the membrane of CCRF-CEM cells.

摘要

一系列苯并(b)噻吩磺酰胺1,1 -二氧化物衍生物(BTS)已被设计并合成为候选抗肿瘤药物。其中几种化合物已显示出对白血病CCRF - CEM细胞的体外细胞毒性活性。具有细胞毒性的BTS,而非无活性的BTS,能够抑制CCRF - CEM细胞膜中存在的肿瘤细胞特异性NADH氧化酶活性。

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