6-芳基氨基-5,8-喹啉二酮和6-氯-7-芳基氨基-5,8-异喹啉二酮对NAD(P)H：醌氧化还原酶（NQO1）活性的影响及其细胞毒性潜力。

Effects of 6-arylamino-5,8-quinolinediones and 6-chloro-7-arylamino-5,8-isoquinolinediones on NAD(P)H: quinone oxidoreductase (NQO1) activity and their cytotoxic potential.

作者信息

Ryu C K, Jeong H J, Lee S K, You H J, Choi K U, Shim J Y, Heo Y H, Lee C O

机构信息

College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seoul 120-750, Korea.

出版信息

Arch Pharm Res. 2001 Oct;24(5):390-6. doi: 10.1007/BF02975181.

DOI:10.1007/BF02975181

PMID:11693537

Abstract

Synthesized 6-arylamino-5,8-quinolinediones 4a-4j and 6-chloro-7-arylamino-5,8-isoquinolinediones 5a-5g were evaluated for effects on NAD(P)H: quinone oxidoreductase (NQO1) activity with the cytosolic fractions derived from cultured human lung cancer cells and their cytotoxicity in cultured several human solid cancer cell lines. The 5,8-quinolinediones 4 and 5,8-isoquinolinediones 5 affected the reduction potential by NQO1 activity and showed a potent cytotoxic activity against human cancer cell lines. The tested compounds 4a, 5c, 5f, and 5g were considered as more potent cytotoxic agents. The compounds 4d, 5b, 5c, 5e and 5g were comparable modulators of NQO1 activity.

摘要

对合成的6-芳基氨基-5,8-喹啉二酮4a - 4j和6-氯-7-芳基氨基-5,8-异喹啉二酮5a - 5g进行了评估，以研究它们对来自培养的人肺癌细胞的胞质部分中NAD(P)H:醌氧化还原酶（NQO1）活性的影响，以及它们在几种培养的人实体癌细胞系中的细胞毒性。5,8-喹啉二酮4和5,8-异喹啉二酮5影响NQO1活性的还原电位，并对人癌细胞系表现出强大的细胞毒性活性。测试的化合物4a、5c、5f和5g被认为是更有效的细胞毒性剂。化合物4d、5b、5c、5e和5g是NQO1活性的类似调节剂。