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

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 in...

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Published inOrganic & biomolecular chemistry Vol. 11; no. 39; pp. 6680 - 6685
Main Authors Babu, PVijaya, Mukherjee, Soumita, Deora, Girdhar Singh, Chennubhotla, Keerthana Sarma, Medisetti, Raghavender, Yellanki, Swapna, Kulkarni, Pushkar, Sripelly, Shivashankar, Parsa, Kishore VL, Chatti, Kiranam, Mukkanti, K, Pal, Manojit
Format Journal Article
LanguageEnglish
Published 01.09.2013
Subjects
Danio rerio
Freshwater
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Summary: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 (IC sub(50) approximately 5-14 mu M) 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.
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ISSN:1477-0520
1477-0539
DOI:10.1039/c3ob41504j