Journal
RSC ADVANCES
Volume 12, Issue 41, Pages 26989-26993Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d2ra04670a
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Funding
- German Cancer Research Center (DKFZ)
- European Molecular Biology Laboratory (EMBL)
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Scalable asymmetric syntheses of two kallikrein-related protease 6 (KLK6) inhibitors were achieved by linking enantiomerically enriched fragments via amide bond formation, followed by conversion of a cyano group to an amidine. X-ray crystallographic analysis of two derivatives clarified the stereochemical outcome of the reaction. X-ray crystallography of the inhibitor complexes bound to human KLK6 revealed their binding poses.
Scalable asymmetric syntheses of two kallikrein-related protease 6 (KLK6) inhibitors are reported. The inhibitors are assembled by linking enantiomerically enriched fragments via amide bond formation, followed by conversion of a cyano group to an amidine. One fragment, an amine, was prepared using the Ellman auxiliary, and a lack of clarity in the literature regarding the stereochemical outcome of this reaction was solved via X-ray crystallographic analysis of two derivatives. Complexes of the inhibitors bound to human KLK6 were solved by X-ray crystallography, revealing the binding poses.
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