title: Synthesis of chalcone derivatives as potential anti-diabetic agents.
abstract: Chalcones bearing electron donating or electron withdrawing substitutions were prepared and their glucose uptake activity was evaluated. Chalcone derivatives were synthesized in one step protocol with high purity and yield. Chalcones with chloro, bromo, iodo and hydroxy substitutions at position 2 on A-ring exhibited the highest activity with glucose medium concentration (210 to 236 mg/dl) compared to pioglitazone and rosiglitazone (230 and 263 mg/dl, respectively). Also chalcones with iodo substitution at position 3 on A-ring were comparably active (≤238 mg/dl). The structure-activity relationship of the tested chalcones was studied and the findings were supported statistically.
authors.affiliation: Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
authors.forename: Chi-Ting
authors.initials: CT
authors.lastname: Hsieh
authors.forename: Tusty-Jiuan
authors.initials: TJ
authors.lastname: Hsieh
authors.forename: Mohamed
authors.initials: M
authors.lastname: El-Shazly
authors.forename: Da-Wei
authors.initials: DW
authors.lastname: Chuang
authors.forename: Yi-Hong
authors.initials: YH
authors.lastname: Tsai
authors.forename: Chiao-Ting
authors.initials: CT
authors.lastname: Yen
authors.forename: Shou-Fang
authors.initials: SF
authors.lastname: Wu
authors.forename: Yang-Chang
authors.initials: YC
authors.lastname: Wu
authors.forename: Fang-Rong
authors.initials: FR
authors.lastname: Chang
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D001693:Biological Transport, Active / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology; D003920:Diabetes Mellitus / Q000188:drug therapy; D005947:Glucose / Q000819:agonists / Q000378:metabolism*; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D000077205:Pioglitazone; D000077154:Rosiglitazone; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000494:pharmacology
chemical_list: D047188:Chalcones; D007004:Hypoglycemic Agents; D045162:Thiazolidinediones; D000077154:Rosiglitazone; D005947:Glucose; D000077205:Pioglitazone