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Synthesis and Biological Studies of a Triazole Analogue of Resorcylic Acid Lactone LL‐Z1640‐2
Author(s) -
Goh Wendy Y. L.,
Chai Christina L. L.,
Chen Anqi
Publication year - 2014
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201403010
Subject(s) - chemistry , natural product , lactone , triazole , stereochemistry , biological activity , enone , yield (engineering) , combinatorial chemistry , chemical synthesis , organic chemistry , biochemistry , in vitro , materials science , metallurgy
Abstract A highly convergent and concise synthesis of a triazole analogue of resorcylic acid lactone natural product LL‐Z1640‐2 has been achieved from easily accessible starting materials in six linear steps in 18 % overall yield. Biological evaluation confirmed the enone system of the natural product is crucial for its activity. The triazole analogue showed good activity (IC 50 7.2 μ M ) against MNK2 kinase, which is an emerging target for cancer chemotherapy.