Fluorescent CDK inhibitors for treatment of cancer

摘要

Disclosed are molecules and their synthesis. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.

主权项

1. A method for synthesizing roscovitine and purvalanol analogs, comprising the steps of: a) providing 2-fluoro-6-chloro-purine; b) functionalizing the N9 position of the purine with a C1-4 alkyl group; c) providing a small aromatic or small heteroaromatic ring system that is substituted with an amino group and with a protected or unprotected group selected from the moieties consisting of carboxylic acid, amide, sulfamide and phosphamide; d) adding the amino group of the small aromatic or small heteroaromatic ring system to the purine C6 position; e) condensing the protected or unprotected group with a linker that is a side chain on a fluorophore moiety, wherein the linker is alkyl, alkenyl, alkynyl, polyalkylamine, alkylene polyamine, sulfoester, phosphoester, amide, sulfamide, or phosphoamide; and f) adding an optionally substituted hydrocarbon amine at the purine C2 position.