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

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• 作者：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
• 关键词：Pyrazoline ; Anticancer ; p53
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：1 December, 2013
• 年：2013
• 卷：21
• 期：23
• 页码：7343-7356
• 全文大小：630 K

文摘

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^{鈭?鈭?/sup> 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.}