2. Academic Validation
  3. Synthesis and SAR studies of bis-chromenone derivatives for anti-proliferative activity against human cancer cells

Synthesis and SAR studies of bis-chromenone derivatives for anti-proliferative activity against human cancer cells

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5256-9. doi: 10.1016/j.bmcl.2014.09.057.
Eeda Venkateswararao 1,  Vinay K Sharma 1,  Manoj Manickam 1,  Jieun Yun 2,  Sang-Hun Jung 3
Affiliations

Affiliations

  • 1 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.
  • 2 Bio-Evaluation Center, KRIBB, Cheongwon-gun Chungcheongbuk-do 363-883, Republic of Korea.
  • 3 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea. Electronic address: jungshh@cnu.ac.kr.
PMID: 25442319 DOI: 10.1016/j.bmcl.2014.09.057
Abstract

A novel family of 3-((4-oxo-4H-chromen-3-yl)methyl)-4H-chromen-4-one (bis-chromone) derivatives were designed, synthesized and studied for their anti-cancer activity using the XTT assay for the growth inhibition against various human Cancer cells. Among them, 3-((5-(cyclohexylmethoxy)-4-oxo-4H-chromen-3-yl)methyl)-7-methoxy-4H-chromen-4-one and 3-((5-(cyclohexylmethoxy)-4-oxo-4H-chromen-3-yl)methyl)-7-hydroxy-4H-chromen-4-one showed micromolar level of in vitro anti-proliferative activity against human Cancer cell lines. The SAR studies indicated bis-chromone as a basic scaffold to design Anticancer agents. The 5-cyclohexylmethoxy on the first chromenone ring and electron donating group such as CH3, OCH3 or hydrogen bonding group (OH) on the Other chromenone ring of bis-chromone increased the activity. However, saturation of one of chromenone to chromanone in bis-chromones decreased the activity.

Keywords

Anti-cancer; Bis-chromone; Cytotoxicity.

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