synthesis and cytotoxic activity of some new 2,6-substituted purines一些新的合成和细胞毒性活动2,6-substituted嘌呤.pdf

Molecules 2011, 16, 5840-5860; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines Nageswara Rao Kode and Shashikant Phadtare * Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA * Author to whom correspondence should be addressed; E-Mail: sphadtar@; Tel.: +1-504-520-5378; Fax: +1-504-520-7954. Received: 20 June 2011 / Accepted: 29 June 2011 / Published: 11 July 2011 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 10µMconcentration. N -[(Z)-4-chloro-2-butenyl-1-yl]- 9 2,6-dichloropurine(5a), N -[4-chloro-2-butynyl- 1-yl]-2,6-dichloropurine(10a), N -[(E)- 9 9 2,3-dibromo-4-chloro-2-butenyl-1-yl]-6-methoxypurine(14)and N -[4-chloro-2-butynyl- 9 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. Keywords: Suzuki-Miyaura cross coupling reac