title: Design and synthesis of chalcone derivatives as potential non-purine xanthine oxidase inhibitors.
abstract: BACKGROUND
  Based on some previous research, the chalcone derivatives exhibited potent xanthine oxidase inhibitory activity, e.g. sappanchalcone (7), with IC50value of 3.9 μM, was isolated fromCaesalpinia sappan. Therefore, objectives of this research are design and synthesis of7and other chalcone derivatives by Claisen-Schmidt condensation and then evaluate their XO inhibitory activity.
  
  
  RESULTS
  Fifteen chalcone derivatives were synthesized by Claisen-Schmidt condensation, and were evaluated for XO inhibitory activity. Nine out of 15 synthetic chalcones showed inhibitory activity (3;5-8;10-13). Sappanchalcone derivatives (11) (IC50, 2.5 μM) and a novel chalcone (13) (IC50, 2.4 μM) displayed strong xanthine oxidase inhibitory activity that is comparable to allopurinol (IC50, 2.5 μM). The structure-activity relationship of these chalcone derivatives was also presented.
  
  
  CONCLUSIONS
  It is the first research on synthesis sappanchalcone (7) by Claisen-Schmidt condensation. The overall yield of this procedure was 6.6 %, higher than that of reported procedure (4 %). Design, synthesis, and evaluation of chalcone derivatives were carried out. This result suggests that the chalcone derivative can be used as potential non-purine XO inhibitors.Graphical abstractThe chalcone derivatives as potential non-purine xanthine oxidase inhibitors.
authors: Faculty of Chemistry, University of Science, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam.
authors: Trung Huu
authors: TH
authors: Bui
authors: Faculty of Chemistry, University of Science, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam ; Cancer Research Laboratory, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam.
authors: Nhan Trung
authors: NT
authors: Nguyen
authors: Faculty of Chemistry, University of Science, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam.
authors: Phu Hoang
authors: PH
authors: Dang
authors: Faculty of Chemistry, University of Science, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam.
authors: Hai Xuan
authors: HX
authors: Nguyen
authors: Faculty of Chemistry, University of Science, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam ; Cancer Research Laboratory, Vietnam National University, 227 Nguyen Van Cu, District 5, Ho Chi Minh City, Vietnam.
authors: Mai Thanh Thi
authors: MT
authors: Nguyen
keywords: Chalcone; Non-purine xanthine oxidase inhibitors; Sappanchalcone