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Title: Synthesis of novel heterocyclic oleanolic acid derivatives with improved antiproliferative activity in solid tumor cells. Author: Leal AS, Wang R, Salvador JA, Jing Y. Journal: Org Biomol Chem; 2013 Feb 13; 11(10):1726-38. PubMed ID: 23381885. Abstract: A series of new oleanane imidazole carbamates, N-acylimidazoles or N-alkylimidazoles were synthesized, characterized and evaluated for their antiproliferative activity in AsPC-1 pancreatic cancer cells. Structure-activity relationship analysis revealed that the N-alkylimidazole 27 was the most active compound with apoptosis induction abilities correlated with upregulation of NOXA and downregulation of Bcl-xL. The antiproliferative activity of compound 27 was further tested in more solid tumor cell lines with IC(50) values lower than 1 μM.[Abstract] [Full Text] [Related] [New Search]