INHIBITION OF RNA-SYNTHESIS INVITRO BY 9-AMINOACRIDINE CARBOXAMIDE ANTITUMOR AGENTS - EFFECTS ON OVERALL RNA-SYNTHESIS AND SYNTHESIS OF THE INITIATING DINUCLEOTIDE

被引:0
作者
PIESTRZENIEWICZ, MK [1 ]
CZYZ, M [1 ]
DENNY, WA [1 ]
GNIAZDOWSKI, M [1 ]
机构
[1] UNIV AUCKLAND,SCH MED,CANC RES LAB,AUCKLAND,NEW ZEALAND
关键词
D O I
暂无
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of 9-aminoacridine carboxamide derivatives of systematically varied structure was assayed in an RNA synthesis in vitro system. Escherichia coli DNA-dependent RNA polymerase and DNA derived from phage T7 or calf thymus were used to measure the effect of the drugs on overall RNA and the initiating dinucleotide (pppApU) syntheses. By means of multiple linear regression analysis it was shown that the inhibition of these reactions depends both on the drug equilibrium binding constant and kinetic parameters of dissociation of drug-DNA complexes.
引用
收藏
页码:299 / 307
页数:9
相关论文
共 25 条
[2]  
AKTIPIS S, 1977, MOL PHARMACOL, V13, P706
[3]   POTENTIAL ANTITUMOR AGENTS .45. SYNTHESIS, DNA-BINDING INTERACTION, AND BIOLOGICAL-ACTIVITY OF TRIACRIDINE DERIVATIVES [J].
ATWELL, GJ ;
BAGULEY, BC ;
WILMANSKA, D ;
DENNY, WA .
JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (01) :69-74
[4]   POTENTIAL ANTITUMOR AGENTS .43. SYNTHESIS AND BIOLOGICAL-ACTIVITY OF DIBASIC 9-AMINOACRIDINE-4-CARBOXAMIDES, A NEW CLASS OF ANTITUMOR AGENT [J].
ATWELL, GJ ;
CAIN, BF ;
BAGULEY, BC ;
FINLAY, GJ ;
DENNY, WA .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (11) :1481-1485
[5]   POTENTIAL ANTI-TUMOR AGENTS .35. QUANTITATIVE RELATIONSHIPS BETWEEN ANTI-TUMOR (L1210) POTENCY AND DNA-BINDING FOR 4'-(9-ACRIDINYLAMINO)METHANESULFON-M-ANISIDIDE ANALOGS [J].
BAGULEY, BC ;
DENNY, WA ;
ATWELL, GJ ;
CAIN, BF .
JOURNAL OF MEDICINAL CHEMISTRY, 1981, 24 (05) :520-525
[6]  
Gale E.F., 1981, MOL BASIS ANTIBIOTIC, P258
[7]   INHIBITION OF DNA-DEPENDENT RNA-SYNTHESIS BY 8-METHOXYPSORALEN [J].
GNIAZDOWSKI, M ;
CZYZ, M ;
WILMANSKA, D ;
STUDZIAN, K ;
FRASUNEK, M ;
PLUCIENNICZAK, A ;
SZMIGIERO, L .
BIOCHIMICA ET BIOPHYSICA ACTA, 1988, 950 (03) :346-353
[8]   THIOL-DEPENDENT INHIBITION OF RNA-SYNTHESIS INVITRO BY ACRIDINES - STRUCTURE-INHIBITION RELATIONSHIPS [J].
GNIAZDOWSKI, M ;
SZMIGIERO, L ;
WILMANSKA, D .
CANCER LETTERS, 1982, 15 (01) :73-79
[9]  
Gniazdowski M, 1985, Postepy Biochem, V31, P53
[10]  
KRIEBARDIS T, 1988, J BIOL CHEM, V263, P6960