Chemical modification of aphidicolin and the inhibitory effects of its derivatives on DNA polymerase α in vitro

Various derivatives of aphidicolin were prepared and their inhibitory effects on purified DNA polymerase alpha in vitro were assayed. Among these derivatives, the new 3 alpha ,17,18-trihydroxyaphidicol-15-ene was as inhibitory as the know 3-deoxy- and 3-oxoaphidicolins. All the other derivatives wit...

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Published inChemical & pharmaceutical bulletin Vol. 35; no. 4; pp. 1641 - 1644
Main Authors HIRANUMA, S, SHIMIZU, T, YOSHIOKA, H, ONO, K, NAKANE, H, TAKAHASHI, T
Format Journal Article
LanguageEnglish
Published Tokyo Maruzen 1987
Subjects
Aphidicolin
Biological and medical sciences
Chemical Phenomena
Chemistry
Diterpenes - pharmacology
DNA Polymerase II - antagonists & inhibitors
General pharmacology
In Vitro Techniques
Medical sciences
Molecular Conformation
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Inhibition
Structure activity relation
DNA polymerase α
In vitro
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Summary:Various derivatives of aphidicolin were prepared and their inhibitory effects on purified DNA polymerase alpha in vitro were assayed. Among these derivatives, the new 3 alpha ,17,18-trihydroxyaphidicol-15-ene was as inhibitory as the know 3-deoxy- and 3-oxoaphidicolins. All the other derivatives with modification of any of the hydroxyl groups of 1 had no effect on the enzyme in vitro. The structure-activity relationships are discussed concerning functionalization on the aphidicolane ring.
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ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.35.1641