title: Synthesis of substituted triazolyl curcumin mimics that inhibit RANKL-induced osteoclastogenesis.
abstract: Some promising new antiresorptive agents of potential utility for treating osteoporosis were uncovered in a curcumin mimics library possessing a substituted triazole moiety, which is synthesized by the Cu(I)-catalyzed Huisgen 1,3-cycloaddition reaction between two azido intermediates (9 and 10) and various alkynes (a-k). A tartarate-resistant acid phosphatase (TRAP) activity assay was carried out with RANKL-induced osteoclastogenesis of mouse monocyte/macrophage RAW264.7 cells; the results indicated that the curcumin mimics derived from intermediate 10 exhibited stronger inhibitory activity than 9. In particular, curcumin mimics 12h, 13c, and 13e strongly inhibited osteoclast differentiation.
authors.affiliation: Department of Biochemistry, Kwandong University College of Medicine, Gangneung, Republic of Korea.
authors.forename: Sang-Kyu
authors.initials: SK
authors.lastname: Park
authors.forename: Sangtae
authors.initials: S
authors.lastname: Oh
authors.forename: Hye Kyoung
authors.initials: HK
authors.lastname: Shin
authors.forename: Seong Hwan
authors.initials: SH
authors.lastname: Kim
authors.forename: Jungyeob
authors.initials: J
authors.lastname: Ham
authors.forename: Jae-Seok
authors.initials: JS
authors.lastname: Song
authors.forename: Seokjoon
authors.initials: S
authors.lastname: Lee
mesh_terms: D000818:Animals; D050071:Bone Density Conservation Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002454:Cell Differentiation / Q000187:drug effects*; D002460:Cell Line; D003474:Curcumin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D020128:Inhibitory Concentration 50; D008264:Macrophages / Q000166:cytology; D051379:Mice; D015394:Molecular Structure; D010010:Osteoclasts / Q000166:cytology* / Q000187:drug effects*; D053245:RANK Ligand / Q000037:antagonists & inhibitors*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D050071:Bone Density Conservation Agents; D053245:RANK Ligand; D014230:Triazoles; D003474:Curcumin