1458658-77-9Relevant academic research and scientific papers
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
Babu, P. Vijaya,Mukherjee, Soumita,Deora, Girdhar Singh,Chennubhotla, Keerthana Sarma,Medisetti, Raghavender,Yellanki, Swapna,Kulkarni, Pushkar,Sripelly, Shivashankar,Parsa, Kishore V. L.,Chatti, Kiranam,Mukkanti,Pal, Manojit
supporting information, p. 6680 - 6685 (2013/10/01)
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.
