| Autor: |
Babu PV; Dr Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India. manojitpal@rediffmail.com., Mukherjee S, Deora GS, Chennubhotla KS, Medisetti R, Yellanki S, Kulkarni P, Sripelly S, Parsa KV, Chatti K, Mukkanti K, Pal M |
| Jazyk: |
angličtina |
| Zdroj: |
Organic & biomolecular chemistry [Org Biomol Chem] 2013 Oct 21; Vol. 11 (39), pp. 6680-5. Date of Electronic Publication: 2013 Aug 29. |
| DOI: |
10.1039/c3ob41504j |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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