Synthesis and biological evaluation of 6-substituted purine and 9-beta-d-ribofuranosyl purine analogues.
6-Substituted purine and 9-beta-d-ribofuranosyl purine analogues were synthesized and their biological activities were evaluated. CD Spectra and thermal melting studies showed that compounds 8, 9, 10 could interact with RNA and DNA in solution. Compound 8 and 10 may bind with RNA single strand and interfere the formation of RNA duplex. Among of these compounds, compound 8 showed middle inhibition on the growth of HeLa cells (70.21%) and HL-60 cells (70.85%) at 10 microM. Comparing to the structures of these synthetic compounds, it may indicate that the sugar moiety and the 6-amino side chain of nucleoside 8 play an important role in the biological activities.
Wang
Jun-Feng
JF
National Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China.
Zhang
Liang-Ren
LR
Yang
Zhen-Jun
ZJ
Zhang
Li-He
LH
D002455:Cell Division / Q000187:drug effects; D002942:Circular Dichroism; D004247:DNA / Q000378:metabolism*; D005562:Formazans; D018922:HL-60 Cells / Q000187:drug effects; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D009690:Nucleic Acid Conformation; D011684:Purine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D012313:RNA / Q000378:metabolism*; D012996:Solutions; D013778:Tetrazolium Salts
D005562:Formazans; D011684:Purine Nucleosides; D012996:Solutions; D013778:Tetrazolium Salts; C079782:MTT formazan; D012313:RNA; D004247:DNA