169687-97-2Relevant articles and documents
Synthetic nucleosides and nucleotides. 40. Selective inhibition of eukaryotic dna polymerase by 9-(β-D-arabinofuranosyl)-2-(p-n-butylanilino) adenine 5'-triphosphate (BuAaraATP) and its 2'-up azido analog: Synthesis and enzymatic evaluations
Tomikawa, Aki,Seno, Masaki,Sato-Kiyotaki, Kunie,Ohtsuki, Chizuru,Hirai, Toshiaki,Yamaguchi, Toyofumi,Kawaguchi, Takeo,Yoshida, Shonen,Saneyoshi, Mineo
, p. 487 - 501 (2007/10/03)
Starting from 2',3',5'-tri-O-acetyl-2-iodoadenosine, 9-(β-D- arabinofuranosyl)-2-(p-n-butylanilino)adenine and its 2'(S)-azido counterparts were synthesized in seven steps. These exhibited only moderate growth-inhibitory effects against mouse leukemic P388 cells (IC50 = 13-24 μM), although 5'-triphosphate derivatives showed strong and selective inhibitory action on calf thymus DNA polymerase α, but not on β- and ε- polymerases from eukaryotes.
Synthesis and biological activities of sugar-modified 2-(p-n- butylanilino)-2'-deoxyadenosine analogues
Yamaguchi,Sato,Saneyoshi
, p. 529 - 532 (2007/10/02)
Several sugar-modified 2-(p-n-butylanilino)-2'-deoxyadenosine analogues, including arabino and 2'(R)-azido-2'-deoxy analogues and their 5'- triphosphates were synthesized. These nucleosides thus obtained exhibited moderate cytotoxicity against P-388 leukemic cells in culture (IC50 = 13- 24 μM). In contrast to above results, the 5'-triphosphates have been shown to exert strong and selective inhibitory effects on mammalian DNA polymerase α (Ki=0.02-0.04 μM).