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<p>Heteroantennary acetylenic derivatives of bile acids, containing hex-5-ynoyl, 4,7,10,13-tetraoxahexadec-15-ynoyl, 4,7,10-trioxatridec-12-ynoyl, and 4,7-dioxadec-9-ynoyl moieties at different positions of the steroid skeleton, were regioselectively synthesized. The cytotoxic properties of the aforementioned compounds against human embryonic kidney HEK293T, human lung fibroblast VA13, breast cancer MCF7, and lung cancer A549 cell lines were studied. Physicochemical parameters of the synthesized bile acid derivatives were calculated to enable estimation of their polarity, total lipophilicity, and aqueous solubility (TPSA, log<i>P</i>, and log<i>S</i>). A correlation was established between the chemical behavior of the synthesized compounds in esterification reactions and their biological activity. The heteroantennary products were evaluated for possible preparation of multivalent tissue-specific ligands and targeted drug delivery systems on their basis.</p>

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Regioselective synthesis of heteroantennary bile acid derivatives projected as precursors for targeted drug delivery systems

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • Yu. R. Pavley,
  • E. Yu. Yamansarov,
  • D. A. Skvortsov,
  • D. A. Ipatova,
  • S. A. Evteev,
  • N. V. Zyk,
  • U. G. Alekseechkina,
  • R. V. Grossman,
  • E. K. Beloglazkina

摘要

Heteroantennary acetylenic derivatives of bile acids, containing hex-5-ynoyl, 4,7,10,13-tetraoxahexadec-15-ynoyl, 4,7,10-trioxatridec-12-ynoyl, and 4,7-dioxadec-9-ynoyl moieties at different positions of the steroid skeleton, were regioselectively synthesized. The cytotoxic properties of the aforementioned compounds against human embryonic kidney HEK293T, human lung fibroblast VA13, breast cancer MCF7, and lung cancer A549 cell lines were studied. Physicochemical parameters of the synthesized bile acid derivatives were calculated to enable estimation of their polarity, total lipophilicity, and aqueous solubility (TPSA, logP, and logS). A correlation was established between the chemical behavior of the synthesized compounds in esterification reactions and their biological activity. The heteroantennary products were evaluated for possible preparation of multivalent tissue-specific ligands and targeted drug delivery systems on their basis.