Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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

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, Young Ho Kim.

Graphical Abstract:


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.

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

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Article Details

VOLUME: 12
ISSUE: 5
Year: 2015
Page: [385 - 392]
Pages: 8
DOI: 10.2174/1570180812666141111235539
Price: $58