Construction of a Meroterpenoid-Like Compounds Library Based on Diversity-Enhanced Extracts

Haruhisa Kikuchi, Kosuke Kawai, Yota Nakashiro, Takayuki Yonezawa, Kumi Kawaji, Eiichi N. Kodama, Yoshiteru Oshima

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1106-1112
Number of pages7
JournalChemistry - A European Journal
Volume25
Issue number4
DOIs
Publication statusPublished - 2019 Jan 18

Keywords

  • chemical library
  • diversity-enhanced extracts
  • drug discovery
  • natural products
  • terpenoids

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry

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