Naseer Muhammad Moazzam, Ahmed Mukhtiar, Hameed Shahid
Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
Chem Biol Drug Des. 2017 Feb;89(2):243-256. doi: 10.1111/cbdd.12818.
Calixarenes, composed of phenolic units linked by methylene bridges at the 2,6-positions, represent a versatile class of macrocyclic compounds in supramolecular chemistry that can host small molecules or ions in their well-defined hydrophobic cavities. In recent years, it has been recognized that this class of compounds has the potential to serve as platform for the design of biological active compounds. Therefore, the calixarenes functionalized with different pharmacophoric groups have been synthesized as target structure by many researchers and were further evaluated for their biological activities. Owing to their promising biological activities such as antiviral, antibacterial, antifungal, and anticancer, the functionalized calixarenes are recently receiving increased attention from pharmaceutical/medicinal chemistry community. In this review, we summarize and discuss the synthetic approaches and the biological potential of functionalized calixarenes, mainly focusing on the selected recent studies for a comprehensive and target-oriented information, which could help in the design and synthesis of new therapeutic agents leading to the development of clinically viable drugs based on these macrocyles.
杯芳烃由在2,6-位通过亚甲基桥相连的酚单元组成,是超分子化学中一类多功能的大环化合物,其结构明确的疏水空腔能够容纳小分子或离子。近年来,人们认识到这类化合物有潜力作为生物活性化合物设计的平台。因此,许多研究人员已合成了用不同药效基团功能化的杯芳烃作为目标结构,并对其生物活性进行了进一步评估。由于其具有抗病毒、抗菌、抗真菌和抗癌等有前景的生物活性,功能化杯芳烃最近受到了药物/ medicinal化学界越来越多的关注。在这篇综述中,我们总结并讨论了功能化杯芳烃的合成方法及其生物潜力,主要聚焦于近期选定的研究,以获取全面且有针对性的信息,这有助于设计和合成新的治疗剂,从而基于这些大环化合物开发出临床上可行的药物。