TAN-1496-A, TAN-1496-C AND TAN-1496-E, DIKETOPIPERAZINE ANTIBIOTICS WITH INHIBITORY ACTIVITY AGAINST MAMMALIAN DNA TOPOISOMERASE-I

被引：50

作者：

FUNABASHI, Y ^{[1
]}

HORIGUCHI, T ^{[1
]}

IINUMA, S ^{[1
]}

TANIDA, S ^{[1
]}

HARADA, S ^{[1
]}

机构：

[1] TAKEDA CHEM IND LTD,DIV PHARMACEUT RES,RES RES,YODOGAWA KU,OSAKA 532,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1994年 / 47卷 / 11期

关键词：

D O I：

10.7164/antibiotics.47.1202

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Fungal metabolites with an epi-oligothiadiketopiperazine structure, TAN-1496 A, C and E, were isolated from the culture broth of Microsphaeropsis sp. FL-16144. Their molecular formulas were determined to be C22H28N2O9S2, C22H28N2O9S3 and C22H28N2O9S4,, respectively. Structures were determined by comparing the NMR data with those of known diketopiperazine antibiotics, sirodesmins. These metabolites inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I but did not affect the decatenation of kinetoplast DNA by calf thymus topoisomerase II at concentration up to 500 mu M. They strongly suppressed the growth of various murine and human tumor cells and induced apoptosis. Moreover, various derivatives were synthesized to investigate the relationship of their functional groups and biological activities.

引用

页码：1202 / 1218

页数：17

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