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Benzofuran hydrazones as potential scaffold in the development of multifunctional drugs: Synthesis and evaluation of antioxidant, photoprotective and antiproliferative activity
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2018-07-02 , DOI: 10.1016/j.ejmech.2018.07.001
Anna Baldisserotto , Monica Demurtas , Ilaria Lampronti , Davide Moi , Gianfranco Balboni , Silvia Vertuani , Stefano Manfredini , Valentina Onnis

New benzofuranhydrazones 3–12 were easily prepared and assayed for their radical-scavenging ability. Hydrazones 3–12 showed different extent antioxidant activity in DPPH, FRAP and ORAC assays. Good antioxidant activity is related to the number and position of hydroxyl groups on the arylidene moiety. High antioxidant activity is showed by the 2-hydroxy-4-(diethylamino)benzylidene derivative 11. Furthermore, hydrazones 3–12 showed photoprotective capacities with satisfactory in vitro SPF as compared to the commercial PBSA sunscreen filter. The antiproliferative effects of the hydrazones 3–12 was tested on erythroleukemia K562 and Colo-38 melanoma human cells. All the compounds showed growth inhibition in the micromolar to sub micromolar concentration range. If taken together these results points to benzofuran hydrazones as potential multifunctional molecules especially in the treatment of neoplastic diseases being the good antioxidant properties of 5, 7 and 11 correlated to their high antiproliferative activity.



中文翻译:

苯并呋喃盐作为多功能药物开发中的潜在支架:抗氧化剂,光保护性和抗增殖活性的合成和评估

可以轻松制备新的苯并呋喃肼3-12,并测定其清除自由基的能力。DP 3–12在DPPH,FRAP和ORAC分析中显示出不同程度的抗氧化活性。良好的抗氧化活性与亚芳基部分上羟基的数量和位置有关。2-羟基-4-(二乙基氨基)亚苄基衍生物11显示出高抗氧化活性。此外,与商业PBSA防晒滤光片相比,3–12显示出令人满意的体外SPF的光保护能力。3–12的抗增殖作用在红白血病K562和Colo-38黑色素瘤人类细胞上进行了测试。所有化合物在微摩尔至亚微摩尔浓度范围内均显示出生长抑制作用。如果一起这些结果指向苯并呋喃腙作为潜在的多官能分子特别是在肿瘤疾病的存在的良好的抗氧化性能的处理5711关联于它们的高的抗增殖活性。

更新日期:2018-07-02
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