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Issue 39, 2013
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Ligand/PTC-free intramolecular Heck reaction: synthesis of pyrroloquinoxalines and their evaluation against PDE4/luciferase/oral cancer cell growth in vitro and zebrafish in vivo

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Abstract

A series of 1,3-disubstituted pyrrolo[2,3-b]quinoxalines has been designed for the potential inhibition of PDE4 without inhibiting luciferase. A ligand/PTC (phase transfer catalyst) free intramolecular Heck cyclization strategy was used to prepare these compounds, some of which showed significant inhibition of PDE4B (IC50 ≈ 5–14 μM) and growth inhibition of oral cancer cells (CAL 27) but not inhibition of luciferase in vitro. They also showed acceptable safety profiles but no apoptosis in zebrafish embryos.

Graphical abstract: Ligand/PTC-free intramolecular Heck reaction: synthesis of pyrroloquinoxalines and their evaluation against PDE4/luciferase/oral cancer cell growth in vitro and zebrafish in vivo

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Publication details

The article was received on 22 Jul 2013, accepted on 02 Aug 2013 and first published on 05 Aug 2013


Article type: Communication
DOI: 10.1039/C3OB41504J
Org. Biomol. Chem., 2013,11, 6680-6685

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    Ligand/PTC-free intramolecular Heck reaction: synthesis of pyrroloquinoxalines and their evaluation against PDE4/luciferase/oral cancer cell growth in vitro and zebrafish in vivo

    P. V. Babu, S. Mukherjee, G. S. Deora, K. S. Chennubhotla, R. Medisetti, S. Yellanki, P. Kulkarni, S. Sripelly, K. V. L. Parsa, K. Chatti, K. Mukkanti and M. Pal, Org. Biomol. Chem., 2013, 11, 6680
    DOI: 10.1039/C3OB41504J

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