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Synthesis and Biological Studies of a Triazole Analogue of Resorcylic Acid Lactone LL‐Z1640‐2

European Journal of Organic Chemistry. 2014-09; 
Wendy Y. L. Goh Christina L. L. Chai Anqi Chen
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Gene Synthesis … 10–15 mg/mL (equivalent to 285–428 μM) and flash‐frozen in liquid nitrogen and stored in buffer at –80 °C. The IMAP 10000‐tp FP assay kit was purchased from Molecular Devices, and JH3 peptide (5‐FAM‐TATKSGSTTKNRFVV‐NH 2 ) was synthesized by GenScript USA Inc … Get A Quote

摘要

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 (IC50 7.2 μM ) against MNK2 kinase, which is an emerging target for cancer chemotherapy.

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