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Construction of a Meroterpenoid‐Like Compounds Library Based on Diversity‐Enhanced Extracts
Author(s) -
Kikuchi Haruhisa,
Kawai Kosuke,
Nakashiro Yota,
Yonezawa Takayuki,
Kawaji Kumi,
Kodama Eiichi. N.,
Oshima Yoshiteru
Publication year - 2019
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201805417
Subject(s) - natural product , diversity (politics) , drug discovery , combinatorial chemistry , chemistry , computational biology , biology , organic chemistry , biochemistry , sociology , anthropology
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.