Insights into drug discovery from natural products through structural modification
Jichao Chen1, Wenlong Li1, Hequan Yao1
1State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
Fitoterapia
|April 29, 2015
Summary
Natural products are vital in drug discovery but often lack druggability. This review highlights how structural modifications improve natural product druggability for medicinal chemistry applications.
Area of Science:
- Medicinal Chemistry
- Natural Product Chemistry
- Drug Discovery
Background:
- Natural products (NPs) are a rich source of lead compounds and pharmacophores.
- NPs are crucial for drug discovery, but often face challenges with druggability.
- Optimizing NPs is essential to bridge the gap between lead compounds and viable drugs.
Purpose of the Study:
- To review strategies for enhancing the druggability of natural products.
- To illustrate how structural modifications can overcome limitations in NP drug development.
- To showcase successful examples of NP druggability optimization.
Main Methods:
- Literature review of natural product modification strategies.
- Analysis of case studies demonstrating successful NP optimization.
- Focus on structure-activity relationships and pharmacokinetic improvements.
Main Results:
- Structural modification is a viable approach to improve NP druggability.
- Optimization can enhance pharmacological activity and pharmacokinetic profiles.
- Several examples demonstrate successful translation of modified NPs into drug candidates.
Conclusions:
- Structural modification is key to unlocking the full therapeutic potential of natural products.
- Targeted modifications can address specific druggability deficits in NPs.
- This strategy is crucial for advancing natural product-derived drugs in medicinal chemistry.
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