超声辅助合成 3,4-二炔取代异香豆素衍生物：鉴定潜在的细胞毒性剂。
Ultrasound Assisted Synthesis of 3,4-Diyne Substituted Isocoumarin Derivatives: Identification of Potential Cytotoxic Agents.
机构信息
Chemistry Division, Department Science and Humanities, Vignan's Foundation for Science Technology and Research, University (VFSTR) University, Vadlamudi, Guntur-522 213, Andhra Pradesh, India.
Department of Chemistry, Krishna University, Machilipatnam-521001, Andhra Pradesh, India.
出版信息
Mini Rev Med Chem. 2018;18(12):1064-1070. doi: 10.2174/1389557518666180117093706.
BACKGROUND
The 3,4-diyne substituted isocoumarins have been designed, synthesized and explored as potential anti-proliferative agents.
METHOD
Ultrasound assisted synthesis of these compounds was carried out by using a three-step method involving (i) Pd/C-Cu catalyzed cross-coupling between the methyl 2-iodobenzoate and buta- 1,3-diynylbenzene followed by (ii) I2-mediated electrophilic cyclization of the resultant 2-(alk-1- ynyl)benzoate ester and (iii) subsequent alkynylation of 4-iodo-3-(phenylethynyl)-isocoumarin under Pd/C-Cu catalysis.
CONCLUSION
The synthesized compounds showed promising growth inhibition when tested against MDA-MB 231 and K562 cancer cell lines.
背景
3,4-二炔取代的异香豆素已被设计、合成并作为潜在的抗增殖剂进行了探索。
方法
通过三步法，使用超声辅助合成这些化合物，包括（i）Pd/C-Cu 催化的甲酯 2-碘苯甲酸与丁-1,3-二炔基苯之间的交叉偶联，接着（ii）碘介导的所得 2-（烷-1-炔基）苯甲酸酯的亲电环化，以及（iii）在 Pd/C-Cu 催化下，4-碘-3-（苯乙炔基）异香豆素的炔基化。
结论
合成的化合物在测试对 MDA-MB 231 和 K562 癌细胞系的生长抑制作用时表现出良好的效果。
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