Synthesis and cytotoxic activity of some new 2,6-substituted purines

Abstract

A seriesof twenty four acyclic unsaturated 2,6-substututed purines 5a-20b were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10?Mconcentration. N 9-[(Z)-4′-chloro-2′-butenyl-1′-yl]-2, 6-dichloropurine(5a), N9-[4′-chloro-2′-butynyl-1′- yl]-2,6-dichloropurine(10a), N9-[(E)-2′,3′-dibromo- 4′-chloro-2′-butenyl-1′-yl]-6-methoxypurine(14)and N 9-[4′-chloro-2′-butynyl-1′-yl]-6-(4-methoxyphenyl) -purine(19)exhibited highly potent cytotoxic activity with GI50 values in the 1-5 μM range for most human tumor cell lines. Other compounds exhibited moderate activity. © 2011 by the authors; licensee MDPI, Basel, Switzerland.