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Synthesis of Hydroxylated Biphenyl Derivatives Bearing an α,β‐Unsaturated Ketone as a Lead Structure for the Development of Drug Candidates against Malignant Melanoma
ChemMedChem ( IF 3.6 ) Pub Date : 2020-12-04 , DOI: 10.1002/cmdc.202000709 Maria Antonietta Dettori 1 , Marina Pisano 2 , Carla Rozzo 2 , Giovanna Delogu 1 , Davide Fabbri 1
ChemMedChem ( IF 3.6 ) Pub Date : 2020-12-04 , DOI: 10.1002/cmdc.202000709 Maria Antonietta Dettori 1 , Marina Pisano 2 , Carla Rozzo 2 , Giovanna Delogu 1 , Davide Fabbri 1
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A small collection of C2‐symmetric hydroxylated biphenyl derivatives featuring an α,β‐unsaturated ketone as a lead structure was prepared, and the capacity of these compounds to act as antiproliferative agents against four human malignant melanoma cell lines was assayed. The prodrug approach was applied in order to improve the delivery of compounds into the cell by modulation of the phenolic hydroxy protecting group. The hydroxylated biphenyl structure bearing an α,β‐unsaturated ketone and a phenolic‐O‐prenylated chain was found to facilitate the delivery of the molecule and interactions with biological targets. Four compounds showed antiproliferative activity resulting in IC50 values in the range of 1.2 to 2.8 μM.
中文翻译：
以α,β-不饱和酮为先导结构的羟基化联苯衍生物的合成，用于开发针对恶性黑色素瘤的候选药物
制备了一小部分以 α,β-不饱和酮为先导结构的 C 2对称羟基化联苯衍生物，并测定了这些化合物作为抗增殖剂对抗四种人类恶性黑色素瘤细胞系的能力。应用前药方法是为了通过调节酚羟基保护基团来改善化合物向细胞的递送。发现带有α,β-不饱和酮和酚-O-异戊二烯化链的羟基化联苯结构有助于分子的传递和与生物靶标的相互作用。四种化合物显示出抗增殖活性，导致 IC 50值在 1.2 至 2.8 μM 的范围内。
更新日期：2020-12-04
中文翻译：
以α,β-不饱和酮为先导结构的羟基化联苯衍生物的合成，用于开发针对恶性黑色素瘤的候选药物
制备了一小部分以 α,β-不饱和酮为先导结构的 C 2对称羟基化联苯衍生物，并测定了这些化合物作为抗增殖剂对抗四种人类恶性黑色素瘤细胞系的能力。应用前药方法是为了通过调节酚羟基保护基团来改善化合物向细胞的递送。发现带有α,β-不饱和酮和酚-O-异戊二烯化链的羟基化联苯结构有助于分子的传递和与生物靶标的相互作用。四种化合物显示出抗增殖活性，导致 IC 50值在 1.2 至 2.8 μM 的范围内。
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