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Abstract <p>In this study, we proposed for the first time a synthetic route to 4-aminomethyl 1,3-dihydroxyacridones and their 5-aza derivatives using Mannich reaction between 1,3-dihydroxyacridones and aliphatic amines. This approach offers several advantages, including high product yields, controllable reaction selectivity, and easy handling of reaction. As a result of this study, five acridone Mannich bases were synthesized, and their anticancer evaluation reveals moderate activity against the HCT 116 colorectal cancer (IC<sub>50</sub> up to 86 μM, SI &gt; 1.1) and HuTu 80 duodenal adenocarcinoma (IC<sub>50</sub> up to 38 μM, SI &gt; 2.7) cell lines.</p>

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Mannich Reaction between 1,3-Dihydroxyacridones and Their 5-Aza Derivatives and Cyclic Amines: A Simple Pathway to New Anticancer Scaffold

  • 期刊论文

  • 发表日期：

    2026年2月13日

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  • Ainur D. Sharapov,
  • Igor A. Khalymbadzha,
  • Victor N. Meshchaninov

摘要

Abstract

In this study, we proposed for the first time a synthetic route to 4-aminomethyl 1,3-dihydroxyacridones and their 5-aza derivatives using Mannich reaction between 1,3-dihydroxyacridones and aliphatic amines. This approach offers several advantages, including high product yields, controllable reaction selectivity, and easy handling of reaction. As a result of this study, five acridone Mannich bases were synthesized, and their anticancer evaluation reveals moderate activity against the HCT 116 colorectal cancer (IC50 up to 86 μM, SI > 1.1) and HuTu 80 duodenal adenocarcinoma (IC50 up to 38 μM, SI > 2.7) cell lines.