CHEMICAL MODIFICATION OF APHIDICOLIN AND THE INHIBITORY EFFECTS OF ITS DERIVATIVES ON DNA POLYMERASE a IN VITRO

Sayoko Hiranuma; Takeshi Shimizu; Hirosuke Yoshioka; Katsuhiko Ono; Hideo Nakane; Taijo Takahashib

doi:10.1248/cpb.35.1641

Sayoko Hiranuma, Takeshi Shimizu, Hirosuke Yoshioka, Katsuhiko Ono, Hideo Nakane, Taijo Takahashib

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Keywords: aphidicolin, tetracyclic diterpene, DNA polymerase α inhibitor, aphidicolin 17-acetate, aphidicolin 17-crotonate, 16, 17, 18-trihydroxyaphidicolan-3-one, aphidicolane-16, 17, 18-triol, 3a, 17, 18-trihydroxy-aphidicol-15-ene, 16, 17

JOURNAL FREE ACCESS

1987 Volume 35 Issue 4 Pages 1641-1644

DOI https://doi.org/10.1248/cpb.35.1641

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Abstract

Various derivatives of aphidicolin (1) were prepared and their inhibitory effects on purified DNA polymerase α in vitro were assayed. Among these derivatives, the new 3α-, 17, 18-trihydroxyaphidicol-15-ene (24) was as inhibitory as the known 3-deoxy-and 3-oxoaphidicolins, (20) and (14). 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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