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

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

Volume: 12 Issue: 5

Author(s): 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 and Young Ho Kim

Affiliation:

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

Abstract: 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 μg/mL. Meanwhile, compound 3l showed selective cytotoxicity against MCF7 and KB with IC₅₀ of 13.7±0.6 and 15.5±0.9 μg/mL, respectively.

Cite this article as:

Anh Le Tuan Hoang, Cuc Thi Nguyen, Yen Hai Pham, Nhiem Xuan Nguyen, Tai Huu Bui, Thao Thi Do, Nam Hoai Nguyen, Minh Van Chau, Kiem Van Phan and Kim Ho Young, Promising Anticancer Drug Candidates Based on the 7-methoxychromone Scaffold: Synthesis and Evaluation of Antiproliferative Activity, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180812666141111235539