Promising Anticancer Drug Candidates Based on the 7-methoxychromone Scaffold: Synthesis and Evaluation of Antiproliferative Activity

作者：Hoang Le Tuan Anh; Nguyen Thi Cuc; Pham Hai Yen; Nguyen Xuan Nhiem; Bui Huu Tai; Do Thi Thao; Nguyen Hoai Nam; Chau Van Minh; Phan Van Kiem^*; Young Ho Kim

来源：Letters in Drug Design and Discovery, 2015, 12(5): 385-392.

DOI：10.2174/1570180812666141111235539

• Anti-cancer activity
• Imidazolidin-4-one
• 7-Methoxychromone
• Paeonol
• Pyrimidine-2,4,6(1H,3H,5H)-trione
• Semi-synthesis

18 chromone derivatives were designed and synthesized from paeonol. All synthetic compounds were evaluated for their anti-proliferative activity towards eight human cancer cell lines including HepG2, HL-60, KB, LLC, LNCaP, LU-1, MCF7, and SW480. Compounds 3g and 3h presented the best cytotoxic effects towards tested cancer cell lines except HepG2. Their IC50 values were ranging from 7.9 +/- 0.4 to 18.9 +/- 1.3 mu g/mL. Meanwhile, compound 3l showed selective cytotoxicity against MCF7 and KB with IC50 of 13.7 +/- 0.6 and 15.5 +/- 0.9 mu g/mL, respectively.

• 出版日期2015