Synthetic nucleosides and nucleotides. 40. Selective inhibition of eukaryotic DNA polymerase alpha by 9-(beta-D-arabinofuranosyl)-2-(p-n-butylanilino) adenine 5'-triphosphate (BuAaraATP) and its 2'-up azido analog: synthesis and enzymatic evaluations.

Tomikawa A, Seno M, Sato-Kiyotaki K, Ohtsuki C, Hirai T, Yamaguchi T, Kawaguchi T, Yoshida S, Saneyoshi M
Nucleosides Nucleotides (1998), Volume 17, Page 487
PubMed entry

Abstract:

Starting from 2',3',5'-tri-O-acetyl-2-iodoadenosine, ...
Starting from 2',3',5'-tri-O-acetyl-2-iodoadenosine, 9-(beta-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 microM), although 5'-triphosphate derivatives showed strong and selective inhibitory action on calf thymus DNA polymerase alpha, but not on beta- and epsilon-polymerases from eukaryotes.

Polymerases:

Human Pol alpha,Human Pol beta,Human Pol epsilon

Topics:

Nucleotide Analogs / Template Lesions, Nucleotide Incorporation

Status:

new topics/pols set partial results complete validated

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