Ultrasound Assisted Synthesis of 3,4-Diyne Substituted Isocoumarin Derivatives: Identification of Potential Cytotoxic Agents

Author(s): Kancharla Suman, Koya Prabhakara Rao, V. Anuradha, Mandava V. Basaveswara Rao*, Manojit Pal*

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 18 , Issue 12 , 2018

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Graphical Abstract:


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.

Keywords: Isocoumarin, Pd/C, coupling, ultrasound, cancer, K562, VEGF.

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Article Details

Year: 2018
Published on: 13 June, 2018
Page: [1064 - 1070]
Pages: 7
DOI: 10.2174/1389557518666180117093706
Price: $65

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