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Molecular Pharmacology, Vol 14, 290-298, Copyright © 1978 by the American Society for Pharmacology and Experimental Therapeutics

Structure-Activity Relationships of Anthracyclines Relative to Effects on Macromolecular Syntheses

S. T. CROOKE 1, V. H. DUVERNAY 1, L. GALVAN 1, and A. W. PRESTAYKO 1

1 Department of Pharmacology. Baylor College of Medicine. Houston, Texas 77030, and Bristol Laboratories, Syracuse, New York 13201

The anthracyclines studied may be divided into two classes on the basis of their effects on DNA and RNA syntheses. Class I anthracyclines-adriamycin, carminomycin, and pyrromycin-inhibit DNA, whole cell RNA, and nucleolar RNA syntheses at approximately comparable concentrations. Class II anthracyclines-aclacinomycin, marcellomycin, and musettamycin-inhibit whole cellular RNA synthesis at 6-7-fold lower concentrations than those required to inhibit DNA synthesis, and nucleolar RNA synthesis at 170-1250-fold lower concentrations than necessary to inhibit DNA synthesis. Structure-activity relationship studies suggest that the presence of di- or trisaccharides confers nucleolar RNA synthesis-inhibitory specificity on anthracyclines. None of the anthracyclines studied had demonstrable effects on processing of preribosomal RNA.

Note:
ACKNOWLEDGMENTS The authors are indebted to Ms. Julie Durantini and Ms. Polly Wischmeier for assistance in the preparation of this manuscript. We also thank Dr. T. Doyle for numerous discussions regarding the chemistry of the anthracyclines and help in preparation of Tables 3 and 4, and Dr. I. Daskal for helpful discussions regarding the morphological manifestations of the anthracyclines. The support and guidance of Dr. Harris Busch are most appreciated. The authors also wish to thank Dr. J. Strong, Dr. I. Daskal, and Dr. Y. C. Choi for reviewing the manuscript.

Submitted on June 29, 1977
Accepted on October 19, 1977




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