1458658-62-2Relevant 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
, 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.
