Synthesis and biological evaluation of pyrazole derivatives as antitumor agents

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题名:	Synthesis and biological evaluation of pyrazole derivatives as antitumor agents
作者:	游懷真;Yu, Huai-Chen
贡献者:	化學學系
关键词:	吡唑;石膽酸;Pyrazole;Lithocholic acid
日期:	2023-07-27
上传时间:	2024-09-19 14:46:06 (UTC+8)
出版者:	國立中央大學
摘要:	吡唑是一個重要的藥理特徵結構和極具意義的特殊骨架，它是一種由五個成員的異環組成的結構，具有強大的藥理特徵，廣泛的治療包括抗炎、抗微生物、抗焦慮、抗癌等。石膽酸本身針對唾液酸轉移酶也有抑制效果，故設計藥物分子的想法是將吡唑合成到石膽酸的結構中，並研究能否達成更佳的抗癌效果。我們合成出了 YHC001-YHC010 的化合物進行藥物毒性的相關生物學評估。其中，YHC001 對於 MDA-MB-231 細胞具有毒性，且針對唾液酸轉移酶亦有抑制效果。未來希望能夠以此結構為基礎更進一步合成出相關的衍生物去測試對於癌細胞的相關治療效果。;Pyrazole serves as a crucial pharmacological feature structure and a remarkably meaningful unique scaffold. It is a structure composed of a five membered heterocycle, possessing potent pharmacological characteristics and a wide range of therapeutic applications, including anti-inflammatory, antimicrobial, anxiolytic and anticancer activities. Lithocholic acid itself exhibits inhibitory effects on sialyltransferase. Therefore, the idea behind designing drug molecules is to incorporate pyrazole into the structure of lithocholic acid to explore the potential for enhanced anticancer effects. We synthesized compounds YHC001 to YHC010 and conducted relevant biological evaluations. Among them, YHC001 demonstrated cytotoxicity against MDA-MB 231 cells and exhibited inhibitory effects on sialyltransferase. In the future, it is hoped that this structure can serve as a basis for further synthesis of related derivatives to evaluate their therapeutic effects on other cancer cells.
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