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Influence of side-chain changes on histone deacetylase inhibitory and cytotoxicity activities of curcuminoid derivatives.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-04-04 , DOI: 10.1016/j.bmcl.2020.127171 La-Or Somsakeesit 1 , Thanaset Senawong 2 , Pakit Kumboonma 3 , Somprasong Saenglee 4 , Arunta Samankul 2 , Gulsiri Senawong 2 , Chavi Yenjai 1 , Chanokbhorn Phaosiri 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-04-04 , DOI: 10.1016/j.bmcl.2020.127171 La-Or Somsakeesit 1 , Thanaset Senawong 2 , Pakit Kumboonma 3 , Somprasong Saenglee 4 , Arunta Samankul 2 , Gulsiri Senawong 2 , Chavi Yenjai 1 , Chanokbhorn Phaosiri 1
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Using curcuminoids as lead compounds, fifty-nine curcuminoid derivatives with different side chains at the phenolic moiety were synthesized. All compounds were investigated for their histone deacetylase (HDAC) inhibitory activities. The potent pan-HDAC inhibitors were further tested against three human cancer cell lines including Hela, HCT116 and MCF-7 with MTT-based assay. The bisethylamide 4z and the mono-sec-butyl derivative 5j manifested good antiproliferative activities against HCT116 cancer cells with the IC50 values as 14.60 ± 1.19 μg/mL and 7.33 ± 0.98 μg/mL, respectively. Molecular docking study of both compounds with Class I HDACs revealed that the compounds might bind tightly to the binding pocket of HDAC2. These findings suggested that these compounds can be putative candidates for the development of anticancer drugs via inhibiting HDACs.
中文翻译：
侧链变化对姜黄素衍生物的组蛋白脱乙酰基酶抑制和细胞毒性活性的影响。
使用姜黄素类化合物作为先导化合物，合成了在酚类部分具有不同侧链的59个姜黄素类衍生物。研究了所有化合物的组蛋白脱乙酰基酶（HDAC）抑制活性。使用基于MTT的测定法进一步测试了有效的pan-HDAC抑制剂对三种人类癌细胞系的攻击，包括Hela，HCT116和MCF-7。双乙酰胺4z和单仲丁基衍生物5j对HCT116癌细胞表现出良好的抗增殖活性，IC50值分别为14.60±1.19μg/ mL和7.33±0.98μg/ mL。两种化合物与I类HDAC的分子对接研究表明，这些化合物可能与HDAC2的结合口袋紧密结合。
更新日期：2020-04-20
中文翻译：
侧链变化对姜黄素衍生物的组蛋白脱乙酰基酶抑制和细胞毒性活性的影响。
使用姜黄素类化合物作为先导化合物，合成了在酚类部分具有不同侧链的59个姜黄素类衍生物。研究了所有化合物的组蛋白脱乙酰基酶（HDAC）抑制活性。使用基于MTT的测定法进一步测试了有效的pan-HDAC抑制剂对三种人类癌细胞系的攻击，包括Hela，HCT116和MCF-7。双乙酰胺4z和单仲丁基衍生物5j对HCT116癌细胞表现出良好的抗增殖活性，IC50值分别为14.60±1.19μg/ mL和7.33±0.98μg/ mL。两种化合物与I类HDAC的分子对接研究表明，这些化合物可能与HDAC2的结合口袋紧密结合。
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