Novel modified purine bases and nucleosides: new methodologies of synthesis and biological activity.
Novel modified purine derivatives (bases or nucleosides) bearing C-substituents in position(s) 6, 2 and/or 8 were prepared by Pd- or Fe-catalyzed cross-coupling reactions of halopurines with organometallics. Reactions of di- and trihalopurines are regioselective and applicable to the synthesis of di- or trisubstituted purines bearing different substituents. Cross-coupling reactions of protected functionalized organometallics were used for the preparation of purines bearing functionalized C-substituents. Some of the title modified purine bases and nucleosides display cytostatic activity.
Hocek
Michal
M
Centre for New Antivirals and Antineoplastics, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, CZ-16610 Prague 6, Czech Republic. hocek@uochb.cas.cz
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009705:Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009942:Organometallic Compounds / Q000737:chemistry; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D009705:Nucleosides; D009942:Organometallic Compounds; D011687:Purines