Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53 |
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| Authors: | Mohammad Abdel-Halim Adam B. Keeton Evrim Gurpinar Bernard D. Gary Simon M. Vogel Matthias Engel Gary A. Piazza Frank M. Boeckler Rolf W. Hartmann Ashraf H. Abadi |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo 11835, Egypt;2. Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, D-66123 Saarbrücken, Germany;3. Mitchell Cancer Institute, University of South Alabama, 1660 Springhill Avenue, Suite 3029, Mobile, AL 36604, United States;4. Department of Pharmacology and Toxicology, The University of Alabama at Birmingham, Birmingham, AL 35294, United States;5. Laboratory for Molecular Design and Pharmaceutical Biophysics, Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Tuebingen, 72074 Tuebingen, Germany |
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| 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 IC50 values in the low micromolar range with a clearly more pronounced effect on the p53+/+ HCT116 cells. The compound class shows excellent developability due to the modular synthesis, allowing independent optimization of all three to four key substituents to improve the properties of the molecules. |
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| Keywords: | Pyrazoline Anticancer p53 |
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