Department of Life Sciences and Biotechnology, University of Ferrara, Via Fossato di Mortara 17-19, Ferrara, I-44121, Italy.
Department of Life and Environmental Sciences, Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, Via Ospedale 72, Cagliari, I-09124, Italy.
Eur J Med Chem. 2018 Aug 5;156:118-125. doi: 10.1016/j.ejmech.2018.07.001. Epub 2018 Jul 2.
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.
新的苯并呋喃腙 3-12 很容易被制备出来，并对其清除自由基的能力进行了测试。腙 3-12 在 DPPH、FRAP 和 ORAC 测定中显示出不同程度的抗氧化活性。良好的抗氧化活性与芳基亚甲基部分上的羟基数目和位置有关。2-羟基-4-(二乙氨基)苯亚甲基衍生物 11 表现出高抗氧化活性。此外，腙 3-12 具有光保护能力，与商业 PBSA 防晒霜相比，在体外 SPF 方面表现出令人满意的效果。腙 3-12 对红白血病 K562 和 Colo-38 黑色素瘤人细胞的增殖抑制作用进行了测试。所有化合物在微摩尔至亚微摩尔浓度范围内均表现出生长抑制作用。如果综合来看，这些结果表明苯并呋喃腙类化合物具有潜在的多功能分子特性，特别是在治疗肿瘤疾病方面，5、7 和 11 的良好抗氧化性能与其高增殖活性有关。
