Synthesis and antitumor activity of tropolone derivatives. 7. Bistropolones containing connecting methylene chains.
Basic Information
ID: ALA1126143
Journal: J Med Chem
Title: Synthesis and antitumor activity of tropolone derivatives. 7. Bistropolones containing connecting methylene chains.
Authors: Yamato M, Ando J, Sakaki K, Hashigaki K, Wataya Y, Tsukagoshi S, Tashiro T, Tsuruo T.
Abstract: Bistropolone derivatives (4-12) containing differing lengths of linkage between the two tropolone rings were prepared and examined for their antitumor activity in in vitro (KB cell) and in vivo (leukemia P388 in mice) systems. Parent compound 3, related compounds previously prepared, and the new compounds 4-12 were evaluated for inhibitory activity against ribonucleotide reductase by indirect means to measure their effects on the dNTP pool imbalance. Present structure-activity relationship results would suggest that potently active bistropolones in vivo inhibit intracellular ribonucleotide reductase through chelating with the two irons at the two active sites of the enzyme.
CiteXplore: 1732542
DOI: 10.1021/jm00080a010
Patent ID: ┄