Natural and Synthetic Lactones Possessing Antitumor Activities
Younghoon Kim1,2, Sandip Sengupta2, Taebo Sim1,2
1KU-KIST Graduate School of Converging Science and Technology, Korea University, 145 Anam-ro, Seongbuk-gu, Seoul 02841, Korea.
Abstract:
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 (4). 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.
Insights
Natural and synthetic lactones show promise as anti-cancer agents. This review explores their anti-tumor activities and synthesis, highlighting L-783277 for oncology drug discovery.
Area of Science:
- Medicinal Chemistry
- Natural Product Chemistry
- Oncology
Background:
- Cancer remains a leading global cause of mortality, necessitating novel therapeutic strategies.
- Lactones, both natural and synthetic, exhibit diverse biological activities, including significant anti-tumor potential.
- Several lactone compounds have been developed as anti-cancer drugs in recent decades.
Purpose of the Study:
- To review the anti-tumor activities and synthetic pathways of natural and synthetic lactones.
- To present research on the chemical modification and biological assessment of resorcylic acid lactone L-783277.
- To underscore the value of lactones as scaffolds in natural product-based oncology drug discovery.
Main Methods:
- Literature review of natural and synthetic lactones with anti-tumor properties.
- Exploration of synthetic routes for lactone compounds.
- Chemical modification and biological evaluation of specific lactone derivatives, exemplified by L-783277.
Main Results:
- Natural and synthetic lactones possess diverse anti-tumor activities.
- Various synthetic strategies exist for producing lactone compounds.
- The resorcylic acid lactone L-783277 has undergone chemical modification and biological assessment.
Conclusions:
- Lactones represent a promising class of compounds for developing new oncology drugs.
- The exploration of lactone scaffolds derived from natural products can accelerate drug discovery.
- Further research into lactone derivatives may yield novel anti-cancer therapeutics.
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