Scholarlink

Abstract <p>An original method was proposed for the synthesis of 5-(cyclopent-1-en-1-yl)-1,2,3-trimethoxybenzene with an overall yield of about 70%. The method involves metallation of 5-bromo-1,2,3-trimethoxybenzene, reaction of the lithium derivative with cyclopentanone, and dehydration using <i>p</i>-toluenesulfonic acid. The corresponding diarylcyclopentene analogs of combretastatins were synthesized via a cross-coupling reaction of this cyclopentene with aryl iodides. The Pd(OAc)<sub>2</sub>/Ag<sub>2</sub>CO<sub>3</sub> catalytic system was found to be effective in this cross-coupling reaction. A significant level of cytotoxicity against HuTu-80, U118, HepG2, and B16 tumor cells was revealed for the cyclopentene analogs of combretastatins (MTT assay).</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Synthesis and Study of the Structure and Cytotoxicity of Five-Membered Cyclic Structural Analogs of Combretastatin A4

  • 期刊论文

  • 发表日期：

    2026年5月25日

查看全文
  • Sergei S. Patrushev,
  • Efim D. Metlitskii,
  • Stepan V. Morozov,
  • Tat’yana V. Rybalova,
  • Marina A. Zenkova,
  • Andrey V. Markov,
  • Elvira E. Shults

摘要

Abstract

An original method was proposed for the synthesis of 5-(cyclopent-1-en-1-yl)-1,2,3-trimethoxybenzene with an overall yield of about 70%. The method involves metallation of 5-bromo-1,2,3-trimethoxybenzene, reaction of the lithium derivative with cyclopentanone, and dehydration using p-toluenesulfonic acid. The corresponding diarylcyclopentene analogs of combretastatins were synthesized via a cross-coupling reaction of this cyclopentene with aryl iodides. The Pd(OAc)2/Ag2CO3 catalytic system was found to be effective in this cross-coupling reaction. A significant level of cytotoxicity against HuTu-80, U118, HepG2, and B16 tumor cells was revealed for the cyclopentene analogs of combretastatins (MTT assay).