A Fast Entry to Furanoditerpenoid-Based Hedgehog Signaling
Inhibitors: Identifying Essential Structural Features
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Abstract
New, small molecule
Hedgehog (Hh) pathway inhibitors, such as the
furanoditerpenoid taepeenin D, are of high medicinal importance. To
establish key structure–activity relationships (SARs) for this
lead, a synthetic sequence has been developed for the expedient preparation
of several derivatives and their evaluation as Hh inhibitors exploiting
its structural similarity to abietic acid. While C(14) substitution
is not essential for biological activity, the presence of a hydrogen
bond acceptor at C(6) and an intact benzofuran moiety are