Synthesis and DNA topoisomerase-II inhibitory activity of unnatural nucleosides.
The synthesis and biological activities of a number of unnatural nucleosides (23-43) is described. Nucleosides have been synthesized by SnCl4-catalyzed condensation of amino sugar acetates and silylated modified pyrimidines. Few of the 2'-O-acetyl derivatives of the nucleosides were hydrolyzed to the respective hydroxy derivatives by treatment with methanol saturated with ammonia. The compounds were screened against Filarial DNA-topoisomerase-II but only one of the compounds (29) inhibited this enzyme at 40 microg/mL of reaction mixture.
Mishra
Ram Chandra
RC
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow, India.
Dwivedi
Namrata
N
Rama
Pati Tripathi
PT
Bansal
Iti
I
Saxena
Jitendra Kumar
JK
D000085:Acetates / Q000737:chemistry; D000641:Ammonia / Q000737:chemistry; D002384:Catalysis; D006868:Hydrolysis; D000432:Methanol / Q000737:chemistry; D009705:Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000378:metabolism; D011743:Pyrimidines / Q000737:chemistry; D017971:Tin Compounds / Q000737:chemistry; D059005:Topoisomerase II Inhibitors
D000085:Acetates; D009705:Nucleosides; D011743:Pyrimidines; D017971:Tin Compounds; D059005:Topoisomerase II Inhibitors; C041694:stannic chloride; D000641:Ammonia; D000432:Methanol