Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53

M Abdel-Halim, AB Keeton, E Gurpinar, BD Gary…

Index: Abdel-Halim, Mohammad; Keeton, Adam B.; Gurpinar, Evrim; Gary, Bernard D.; Vogel, Simon M.; Engel, Matthias; Piazza, Gary A.; Boeckler, Frank M.; Hartmann, Rolf W.; Abadi, Ashraf H. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 23 p. 7343 - 7356

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Abstract

Abstract Derivatives with scaffolds of 1, 3, 5-tri-substituted pyrazoline and 1, 3, 4, 5-tetra- substituted pyrazoline were synthesized and tested for their inhibitory effects versus the p53+/+ HCT116 and p53−/− H1299 human tumor cell lines. Several compounds were active against the two cell lines displaying IC 50 values in the low micromolar range with a clearly more pronounced effect on the p53+/+ HCT116 cells. The compound class shows ...