1548331-46-9Relevant academic research and scientific papers
Synthesis and Cytotoxic Evaluation of Monocarbonyl Analogs of Curcumin as Potential Anti-Tumor Agents
Pan, Zheer,Chen, Chengwei,Zhou, Yeli,Xu, Feng,Xu, Yaozeng
, p. 43 - 49 (2016/02/23)
(Table Presented) A series of mono-carbonyl curcumin analogs with different substituents at the 4/4′-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines using a methyl thiazolyl tetrazolium assay. Several of the curcumin analogs, especially B114, exhibited a wide-spectrum of anti-tumor properties in all tested cell lines, indicating their potential in as anti-cancer lead compounds. Further toxicity testing in the NRK-52E kidney cell line revealed that the analogs A111, A113, and B114 had comparable or higher safety than curcumin. These data suggested that the introduction of appropriate substituents in the 4/4′-positions could be a promising approach for curcumin-based drug design.
Synthesis and biological evaluation of allylated and prenylated mono-carbonyl analogs of curcumin as anti-inflammatory agents
Liu, Zhiguo,Tang, Longguang,Zou, Peng,Zhang, Yali,Wang, Zhe,Fang, Qilu,Jiang, Lili,Chen, Gaozhi,Xu, Zheng,Zhang, Huajie,Liang, Guang
, p. 671 - 682 (2014/03/21)
Curcumin has been shown to possess anti-inflammatory activities but has been limited for its low stability and poor bioavailability. We have previously reported four series of 5-carbon linker-containing mono-carbonyl analogs of curcumin (MACs). In continuation of our ongoing research, we designed and synthesized 33 novel allylated or prenylated MACs here, and evaluated their anti-inflammatory effects in RAW 264.7 macrophages. A majority of them effectively inhibited the LPS-induced expression of TNF-α and IL-6, especially IL-6. The preliminary SAR and quantitative SAR analysis were conducted. Compound 14q is the most potent analog among them, and exhibits significant protection against LPS-induced death in septic mice. Together, these data present a series of new analogs of curcumin as promising anti-inflammatory agents.
