药效团
香豆素
生物活性
混合的
组合化学
化学
小分子
药品
计算生物学
合理设计
药理学
体外
生物化学
生物
有机化学
遗传学
植物
作者
Ioannis Fotopoulos,Dimitra Hadjipavlou‐Litina
出处
期刊:Medicinal Chemistry
[Bentham Science Publishers]
日期:2019-04-17
卷期号:16 (3): 272-306
被引量:26
标识
DOI:10.2174/1573406415666190416121448
摘要
Coumarins exhibit a plethora of biological activities, e.g. antiinflammatory and anti-tumor. Molecular hybridization technique has been implemented in the design of novel coumarin hybrids with several bioactive groups in order to obtain molecules with better pharmacological activity and improved pharmacokinetic profile.Therefore, we tried to gather as many as possible biologically active coumarin hybrids referred in the literature till now, to delineate the structural characteristics in relation to the activities and to have a survey that might help the medicinal chemists to design new coumarin hybrids with drug-likeness and varied bioactivities.The biological activities of the hybrids in most of the cases were found to be different from the biological activities presented by the parent coumarins. The results showed that the hybrid molecules are more potent compared to the standard drugs used in the evaluation experiments.Conjugation of coumarin with varied pharmacophore groups/druglike molecules responsible for different biological activities led to many novel hybrid molecules, with a multitarget behavior and improved pharmacokinetic properties.
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