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Synthesis and biological evaluation of O-alkylated tropolones and related alpha-ketohydroxy derivatives as ribonucleotide reductase inhibitors.

作者信息

Tamburlin-Thumin I, Crozet M P, Barrière J C, Barreau M, Riou J F, Lavelle F

机构信息

LCMO, UMR 6517, CNRS Universités d'Aix-Marseille 1 et 3, Av. Escadrille Normandie-Niemen, BP 562, F-13397 Cedex 20, Marseille, France.

出版信息

Eur J Med Chem. 2001 Jun;36(6):561-8. doi: 10.1016/s0223-5234(01)01249-1.

DOI:10.1016/s0223-5234(01)01249-1
PMID:11525847
Abstract

A series of O-alkylated tropolones and related alpha-ketohydroxy compounds were evaluated for their biological activities and were shown to present an expected ribonucleotide reductase inhibition and cytotoxicity against some cancer cell lines but no antitubulin activity. Pharmacomodulation studies were realised to understand and enhance the observed activities. These original benzylic, heterocyclic and allylic compounds have been synthesised by a phase-transfer catalysed O-alkylation developed in our laboratories.

摘要

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