KU-KIST Graduate School of Converging Science and Technology, Korea University, 145 Anam-ro, Seongbuk-gu, Seoul 02841, Korea.
Severance Biomedical Science Institute, Graduate School of Medical Science (Brain Korea 21 Project), College of Medicine, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Korea.
Int J Mol Sci. 2021 Jan 21;22(3):1052. doi: 10.3390/ijms22031052.
Cancer is one of the leading causes of death globally, accounting for an estimated 8 million deaths each year. As a result, there have been urgent unmet medical needs to discover novel oncology drugs. Natural and synthetic lactones have a broad spectrum of biological uses including anti-tumor, anti-helminthic, anti-microbial, and anti-inflammatory activities. Particularly, several natural and synthetic lactones have emerged as anti-cancer agents over the past decades. In this review, we address natural and synthetic lactones focusing on their anti-tumor activities and synthetic routes. Moreover, we aim to highlight our journey towards chemical modification and biological evaluation of a resorcylic acid lactone, L-783277 (). We anticipate that utilization of the natural and synthetic lactones as novel scaffolds would benefit the process of oncology drug discovery campaigns based on natural products.
癌症是全球主要死亡原因之一,每年估计有 800 万人因此死亡。因此,迫切需要发现新的肿瘤药物。天然和合成内酯具有广泛的生物学用途,包括抗肿瘤、抗寄生虫、抗微生物和抗炎活性。特别是,在过去几十年中,几种天然和合成内酯已成为抗癌药物。在这篇综述中,我们重点介绍了天然和合成内酯,关注它们的抗肿瘤活性和合成途径。此外,我们旨在强调我们在化学修饰和生物评价方面的进展,以一种雷琐酚内酯,L-783277()为模型。我们预计,利用天然和合成内酯作为新型支架将有助于基于天然产物的肿瘤药物发现活动。