Synthesis of 6-Aryl-Substituted Derivatives of 8-Acetylharmine and Evaluation of Their Cytotoxicity and Antidepressant Activity

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发表日期：

2024年11月8日

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A. Amanzhan,
V. A. Savelyev,
O. V. Maslova,
Zh. B. Iskakova,
E. E. Shults,
S. M. Adekenov

摘要

Bromination by N-bromosuccinimide of the β-carboline alkaloid 8-acetylharmine in CH₂Cl₂ smoothly formed 8-acetyl-6-bromoharmine. Cross coupling of 8-acetyl-6-bromoharmine with arylboronic acids in aqueous toluene in the presence of Pd(PPh₃)₄ as a catalyst, Na₂CO₃ as a base, and ammonium salt Bu₄N⁺Br^- as an additive synthesized the corresponding 6-aryl-8-acetylharmine derivatives. The new aryl-substituted 8-acetylharmine derivatives possessed moderate cytotoxicity and antidepressant activity in the Porsolt test.