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Claims for Patent: 5,661,136

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Claims for Patent: 5,661,136

Title: 2-halo-2'-fluoro ARA adenosines as antinoplastic agents
Abstract:The present invention is directed to certain 2'-fluoro, 2-substituted purine nucleosides which are toxic to cancerous cell lines.
Inventor(s): Montgomery; John A. (Birmingham, AL), Secrist, III; John A. (Birmingham, AL)
Assignee: Southern Research Institute (Birmingham, AL)
Application Number:08/320,879
Patent Claims: 1. A method for bringing about a cytotoxic effect in a mammalian cancerous cell which comprises contacting said cancerous cell with an effective amount of a cytotoxic compound having the formula ##STR6## wherein R, each which may be the same or different, is hydrogen or a protecting group; wherein Z is a selected from the group consisting of F, Cl, and Br; and pharmaceutically acceptable salts thereof.

2. A method according to claim 1 which comprises contacting said cancerous cell with a compound wherein R is a protecting group.

3. A method according to claim 1 which comprises contacting said cancerous cell with compound wherein R is hydrogen.

4. A method according to claim 1 which comprises contacting said cancerous cell with a compound wherein Z is Cl.

5. A method according to claim 1 which comprises contacting said cancerous cell with a compound wherein the compound is 2-Chloro-9-(2-deoxy-2- fluoro-.beta.-D-arabinofuranosyl)-9H-purin-6-amine.

6. A method for inhibiting ribonucleotide reductase and DNA polymerase .alpha. in a mammalian cell which comprises contacting said mammalian cell with of a cytotoxic compound having the formula ##STR7## wherein R, each which may be the same or different, is hydrogen or a protecting group; wherein Z is a halogen selected from the group consisting of F, Cl, and Br; and pharmaceutically acceptable salts thereof.

7. A method according to claim 6 wherein R of said compound is a protecting group.

8. A method according to claim 6 wherein R of said a compound is hydrogen.

9. A method for inhibiting ribonucleotide reductase and DNA polymerase .alpha. in a mammalian cell which comprises contacting said mammalian cell with of a cytotoxic compound having the formula ##STR8## wherein R, each which may be the same or different, is hydrogen or a protecting group; wherein Z is a halogen selected from the group consisting of F, Cl, and Br; and the pharmaceutically acceptable salts thereof.

10. A method according to claim 9 wherein R of said compound is a protecting group.

11. A method according to claim 9 wherein R of said compound is hydrogen.

12. A method according claim 9 wherein said compound is 2- Chloro-9-(2-deoxy-2-fluoro-.beta.-D arabinofuranosyl)-9H-purin-6-amine.
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