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From Target-Oriented to Motif-Oriented: A Case Study on Nannocystin Total Synthesis
1The State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300353, China.
Molecules (Basel, Switzerland)
|November 18, 2020
Summary
Natural product synthesis requires flexible strategies. Motif-oriented synthesis enables structural diversification for drug discovery, complementing traditional target-oriented approaches.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Drug Discovery
Background:
- Natural product total synthesis initially focuses on constructing a target molecule.
- Subsequent efforts aim for structural diversification to explore structure-activity relationships (SAR).
- Established synthetic routes may lack flexibility for exploring diverse chemical space around specific substructures.
Purpose of the Study:
- To review seven nannocystin total syntheses.
- To compare target-oriented and motif-oriented synthetic strategies.
- To highlight the complementary roles of these strategies in natural product drug discovery.
Main Methods:
- Examination of seven published nannocystin total syntheses.
- Analysis of synthetic strategies employed, focusing on flexibility and diversification.
- Comparison of target-oriented and motif-oriented approaches.
Main Results:
- Demonstrated the utility of motif-oriented strategy for synthesizing varied nannocystins.
- Showcased the limitations of conventional routes in achieving diversification.
- Highlighted the successful application of both strategies in synthesizing nannocystins.
Conclusions:
- Motif-oriented strategy offers superior synthetic flexibility for diversification.
- Target-oriented and motif-oriented strategies are complementary and essential for drug discovery.
- Both approaches are indispensable for advancing natural product-based drug discovery.
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