Intercalating agents specifying nucleotides

• US 4,547,569 A
• Filed: 06/14/1984
• Issued: 10/15/1985
• Est. Priority Date: 11/24/1982
• Status: Expired due to Fees

• Current Assignee: United States Department Of Health And Human Services
• Original Assignee: United States Department Of Health And Human Services
• Inventors: Schott, Margaret E., Letsinger, Robert L.
• Primary Examiner(s): Brown, Johnnie R.
• Assistant Examiner(s): Peselev, Elli
• Application Number:
  US06/620,801
• Time in Patent Office: 488 Days
• Field of Search: 536/23, 536/27, 536/28, 536/29
• US Class Current: 536/25.32
• CPC Class Codes: C07H 21/00 Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
• CPC Class Codes: C12Q 1/68 involving nucleic acids

Abstract

This invention discloses a molecule bearing a biologically active group (a phenanthridinium moiety) joined covalently to an oligonucleotide recognition system (a phosphorus nucleoside group) by a linker that permits intercalation of the active group in the pocket formed by the nucleotide and complementary bases in another polynucleotide strand. This class of compounds is illustrated by the following: ##STR1## where R is selected from the group consisting of --NH₂, methylamino, or ethylamino or hydrogen;

where R'"'"' is selected from the group consisting of --NH₂, methylamino, or ethylamino or hydrogen;

where the chain linking the linker group to the phenanthridinium group (R") consists of 2-8 --CH₂ -- groups.

Claims

1. The compound of the formula ##STR8## where R is selected from the group consisting of --NH₂, methylamino, or ethylamino or hydrogen;

where R'"'"' is selected from the group consisting of --NH₂, methylamino, or ethylamino or hydrogen;

where the chain linking the linker group to the phenanthridinium group (R") consists of 2-8 --CH₂ --groups;

where Th is thymidylyl thymidine; and

where n is an integer from 0-19.

3. The compound of claim 1 which consists of 2 phosphorus nucleosides.

2. The compound of the formula:

##STR9## where Th is thymidylyl thymidine.