| 摘要 |
<p>Disclosed are nitro-substituted squaraine reporter dyes and methods using such dyes for detecting nitroreductase enzyme activity and nitroreductase gene expression in cellular assays. The dyes are of the structure: formula (I) in which Z<1> and Z<2> independently represent a phenyl or a naphthyl ring system; X and Y are selected from oxygen, sulphur, -CH=CH- and the group: formula (A) ; R<1> and R<2> are selected from C1-C4 alkyl, -(CH2)n-P, -{(CH2)2-O}p-R<6> and group W; where P is selected from COOR<7>, SO3- and OH, W is mono- or di-substituted nitrobenzyl, R<6> is methyl or ethyl, R<7> is selected from H, C1-C4 alkyl and CH2OC(O)R<8>, where R<8> is methyl, or t-butyl, n is an integer from 1 to 10, and p is an integer from 1 to 3; R<3> and R<4> are selected from hydrogen, NO2, halogen, SO3-, C1-C4 alkoxy and -(CH2)m-COOR<7>; where R<7> is hereinbefore defined and m is 0 or an integer from 1 to 5; R<5> is C1-C6 alkyl optionally substituted with COOR<7>, SO3-, or OH; where R<7> is hereinbefore defined; and at least one of groups R<1>, R<2>, R<3> and R<4> comprises at least one NO2 group. Also provided are methods for screening for a test agent whose effect upon nitroreductase enzyme activity and nitroreductase gene expression is to be determined.</p> |
