期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 25, 期 4, 页码 1106-1112出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201805417
关键词
chemical library; diversity-enhanced extracts; drug discovery; natural products; terpenoids
资金
- Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan [16H03279, 16H05346]
- Platform Project for Supporting in Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) [JP18am0101095/ JP18am0101100]
- Practical Research for Innovative Cancer Control from AMED [JP17ck0106282/ JP18ck0106282]
- Shorai Foundation for Science and Technology
- Kobayashi International Scholarship Foundation
- Takeda Science Foundation
- Suzuken Memorial Foundation
- Uehara Memorial Foundation
- Grants-in-Aid for Scientific Research [16H03279, 16H05346] Funding Source: KAKEN
The structural diversity of natural products and their derivatives have long contributed to the development of new drugs. However, the difficulty in obtaining compounds bearing skeletally novel structures has recently led to a decline of pharmaceutical research into natural products. This paper reports the construction of a meroterpenoid-like library containing 25 compounds with diverse molecular scaffolds obtained from diversity-enhanced extracts. This method constitutes an approach for increasing the chemical diversity of natural-product-like compounds by combining natural product chemistry and diversity-oriented synthesis. Extensive pharmacological screening of the library revealed promising compounds for anti-osteoporotic and anti-lymphoma/leukemia drugs. This result indicates that the use of diversity-enhanced extracts is an effective methodology for producing chemical libraries for the purpose of drug discovery.
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