Intercalators having affinity for dna and methods of use

C - Chemistry – Metallurgy – 07 – D

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C07D 221/12 (2006.01) C07D 219/14 (2006.01) C07D 401/02 (2006.01) C07D 403/06 (2006.01) C07D 413/06 (2006.01) C07D 413/14 (2006.01) C07D 417/06 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2162382

Intercalator compounds are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment. The intercalator compounds comprise an I moiety bonded to one or more T moieties, said T moieties, when more than one said T moiety are present, are the same or different from one another, said compound having a formula I-(T)m wherein m is an integer from 1 to 5; wherein said 1 moiety is selected from the group consisting of: (see formula I); said T moiety is selected from the group consisting of: (see formula II).

Composés d'intercalation constitués de fractions d'intercalation, ou de fractions d'intercalation substituées, comprenant une ou plusieurs chaînes fonctionnalisées, ou fractions, ces composés se caractérisant par une forte affinité pour se lier à la molécule d'ADN et une faible auto-extinction tout en produisant une cinétique de transport de haut niveau. On a découvert que ces composés produisent une meilleure fluorescence lorsqu'ils sont liés à une molécule d'ADN dans un environnement de cytométrie en flux fluorescent, dont la fluorescence est huit à dix fois supérieure à celle d'agents d'intercalation classiques à structure "bis" et d'autres agents d'intercalation connus utilisés dans un environnement de cytométrie en flux.

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