In this study, we explored Heck- and Suzuki-coupling methodology to modify the template 2,5-di--butylhydroquinone (BHQ, ), an inhibitor of the enzyme sarco/endoplasmic reticulum calcium ATPase (SERCA). We found that by utilizing Suzuki coupling, we could successfully attach a six-carbon tether to BHQ that terminated in a leucine moiety to obtain target . Similar to related compounds based on the structure of the natural product thapsigargin, displayed inhibitory potency against SERCA activity. This makes a suitable candidate for the future attachment of a deactivating peptide to convey specificity for prostate cancer cells.
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| http://dx.doi.org/10.3762/bjoc.15.94 | DOI Listing |
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