title: A fast entry to furanoditerpenoid-based Hedgehog signaling inhibitors: identifying essential structural features.
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.
authors.affiliation: NCSR "Demokritos", P.O. Box 60228, GR-153 10 Ag. Paraskevi, Athens, Greece.
authors.forename: Maria
authors.initials: M
authors.lastname: Chatzopoulou
authors.forename: Antonia
authors.initials: A
authors.lastname: Antoniou
authors.forename: Emmanuel N
authors.initials: EN
authors.lastname: Pitsinos
authors.forename: Marina
authors.initials: M
authors.lastname: Bantzi
authors.forename: Sofia D
authors.initials: SD
authors.lastname: Koulocheri
authors.forename: Serkos A
authors.initials: SA
authors.lastname: Haroutounian
authors.forename: Athanassios
authors.initials: A
authors.lastname: Giannis
mesh_terms: D000045:Acacia / Q000737:chemistry; D001572:Benzofurans / Q000737:chemistry; D053823:Hedgehog Proteins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D015398:Signal Transduction; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001572:Benzofurans; D053823:Hedgehog Proteins; D013729:Terpenes; C550051:taepeenin D; C105430:benzofuran