98 エンジイン化合物の合成とDNA切断(ポスター発表の部)

概要

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The new class of antitumor antibiotics esperamicins, calicheamicins, and dynemicin A have attracted considerable attention due to their very high biological activity as well as their potent DNA cleaving activities. We synthesized sulfur containing macrocyclic enediyne compounds (8,11,20,22 and 23) related to above antibiotics and studied on their radical producing reactions. Enediyne 8 and 11 required long reaction time and high temperature to aromatize under neutral conditions, whereas the sulfone 11 cyclized easily to afford benzenoid adduct 14 in the presence of basic catalysts.(table 1) The sulfone derivative 11 exhibited relatively potent activities depending on the drug concentration, reaction time, and pH. In order to develop more powerful agents, we synthesized the hydroxy derivative 34, in which the hydoxy group would be a connecting functionality with suitable DNA binding molecules.
天然有機化合物討論会の論文
1992-09-10