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<p>A previously unreported macrodiolide featuring a (<i>Z</i>,<i>Z</i>)-1,5-diene moiety was synthesized stereoselectively by Cp<sub>2</sub>TiCl<sub>2</sub>-catalyzed homocyclomagnesiation of functionally substituted 1,2-dienes. Subsequent Ru-catalyzed oxidative cyclization of 1,5-diene bonds within the macrocycle enabled the first synthesis of macrocyclic lactones incorporating 2,5-disubstituted tetrahydrofuran moieties as a pharmacophore. The anticancer activity of the obtained macrocyclic compounds was evaluated against Jurkat, A549, and HEK293 cell lines. The mechanism of action is proposed to be mediated by the ionophore effect of these compounds.</p>

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A new strategy for the design of macrocycles containing tetrahydrofuran pharmacophores with anticancer activity

  • 期刊论文

  • 发表日期：

    2026年2月1日

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  • V. A. D’yakonov,
  • L. U. Dzhemileva,
  • I. I. Islamov,
  • E. Kh. Makarova,
  • I. V. Gaisin,
  • A. A. Makarov,
  • U. M. Dzhemilev

摘要

A previously unreported macrodiolide featuring a (Z,Z)-1,5-diene moiety was synthesized stereoselectively by Cp2TiCl2-catalyzed homocyclomagnesiation of functionally substituted 1,2-dienes. Subsequent Ru-catalyzed oxidative cyclization of 1,5-diene bonds within the macrocycle enabled the first synthesis of macrocyclic lactones incorporating 2,5-disubstituted tetrahydrofuran moieties as a pharmacophore. The anticancer activity of the obtained macrocyclic compounds was evaluated against Jurkat, A549, and HEK293 cell lines. The mechanism of action is proposed to be mediated by the ionophore effect of these compounds.