Indole-based melatonin analogues: Synthetic approaches and biological activity.
Indole-based melatonin analogues: Synthetic approaches and biological activity.
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DOI：
10.1016/j.ejmech.2019.111847
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发表时间：
2019-11
影响因子：
6.7
通讯作者：
Su-Yan Wang;Xin-Chi Shi;P. Laborda
中科院分区：
文献类型：
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作者：
Su-Yan Wang;Xin-Chi Shi;P. Laborda
褪黑激素是一种天然激素，主要由松果体释放，调节睡眠-觉醒周期。褪黑激素的多种生物学应用，以及开发新的褪黑激素能配体的需要，刺激了褪黑激素衍生物的制备。本文综述了吲哚类褪黑激素类似物的合成方法及其生物学应用。已经进行的褪黑激素的吲哚环上的修饰和这些修饰的生物活性的影响进行了分析，详细说明褪黑激素受体的衍生物的结合亲和力。
Melatonin is a natural hormone primarily released by the pineal gland that regulates the sleep-wake cycles. The diverse biological applications of melatonin, together with the need to develop new melatoninergic ligands, have stimulated the preparation of a wide range of melatonin derivatives. Here, all the synthetic approaches to indole-based melatonin analogues as well as their biological applications are reviewed. The modifications which have been performed on the melatonin’s indole ring and the effects of these modifications on the biological activities have been analysed, detailing the binding affinity of the derivatives for melatonin receptors.