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INAUHZIN ANALOGUES THAT INDUCE P53, INHIBIT CELL GROWTH, AND HAVE ANTITUMOR ACTIVITY
INAUHZIN ANALOGUES THAT INDUCE P53, INHIBIT CELL GROWTH, AND HAVE ANTITUMOR ACTIVITY
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机译:诱导P53,抑制细胞生长并具有抗肿瘤活性的类似物
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摘要
Inauhzin (INZ) was identified as a novel p53 activator, which selectively and efficiently suppressing tumor growth without displaying genotoxicity and with little toxicity to normal cells. A panel of INZ analogs were synthesized and evaluated their ability to induce cellular p53 and to inhibit cell growth in cell-based assays. As described, this leads to the discovery of INZ analog 37, a molecule that exhibits much better potency than INZ in both of p53 activation and cell growth inhibition in several human cancer cell lines including H460 and HCT116+/+ cells. This INZ analog exhibited a much lower effect on p53-null H1299 cells and importantly no toxicity towards normal human p53-containing WI-38 cells. Those results also reveal key chemical features for INZ activity, and identify the newly synthesized INZ analog 37 as a better small molecule for further development of anti-cancer therapies.
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