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Ligand-free Pd-catalyzed C–N cross-coupling/cyclization strategy: An unprecedented access to 1-thienyl pyrroloquinoxalines for the new approach towards apoptosis

Ligand-free Pd-catalyzed C–N cross-coupling/cyclization strategy: An unprecedented access to 1-thienyl pyrroloquinoxalines for the new approach towards apoptosis

30 10 2014

Authors: Sunder Kumar Kolli, Ali Nakhi, Sivakumar Archana, Maneesha Saridena, Girdhar Singh Deora, Swapna Yellanki, Raghavender Medisetti, Pushkar Kulkarni, R Ramesh Raju, Manojit Pal

Journal: European Journal of Medicinal Chemistry

Volume: 86 | Issue: | Pages: 270-278

Publisher: Elsevier Masson

researchblogdrsunderligandfreepdcatalyzedcrosscouplingcyclizationstrategyunprecedentedaccess1thienylpyrroloquinoxalinesapproachtowardsapoptosis

The link between PDE4 and apoptosis prompted us to design and synthesize for the first time a series of novel 1-thienyl pyrroloquinoxalines as potential PDE4 inhibitors/apoptotic agents. A ligand-free Pd-catalyzed C–N cross-coupling/cyclization strategy has been developed for the rapid and milder access to this class of compounds some of which showed interesting pharmacological properties when tested in vitro and in zebrafish embryos.

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