title: Synthesis and biological evaluation of a series of tangeretin-derived chalcones.
abstract: A series of chalcones polyoxygenated on the ring A (with pentamethoxy or 2'-hydroxy-3',4',5',6'-tetramethoxy substitution patterns) was synthesized from tangeretin, a natural Citrus flavonoid. These chalcones were evaluated for their antiproliferative, activation of apoptosis, inhibition of tubulin assembly and antileishmanial activities. Comparison with the reference analogous 3',4',5'-trimethoxylated chalcones showed that such peroxygenated substitution patterns on the ring A were less beneficial to these activities.
authors.affiliation: Faculté de Pharmacie, Laboratoire de Pharmacognosie, Univ Paris-Sud 11, BIOCIS, UMR-8076 CNRS, Châtenay-Malabry Cedex, France.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Quintin
authors.forename: Julie
authors.initials: J
authors.lastname: Desrivot
authors.forename: Sylviane
authors.initials: S
authors.lastname: Thoret
authors.forename: Patrick
authors.initials: P
authors.lastname: Le Menez
authors.forename: Thierry
authors.initials: T
authors.lastname: Cresteil
authors.forename: Guy
authors.initials: G
authors.lastname: Lewin
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D047309:Flavones / Q000737:chemistry*; D006801:Humans; D007891:Leishmania / Q000187:drug effects; D010936:Plant Extracts; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D047188:Chalcones; D047309:Flavones; D010936:Plant Extracts; D014404:Tubulin; C059006:tangeretin