2. Academic Validation
  3. Synthesis and antiproliferative activities of quebecol and its analogs

Synthesis and antiproliferative activities of quebecol and its analogs

  • Bioorg Med Chem Lett. 2013 Oct 1;23(19):5329-31. doi: 10.1016/j.bmcl.2013.07.058.
Kasiviswanadharaju Pericherla 1,  Amir Nasrolahi Shirazi,  V Kameshwara Rao,  Rakesh K Tiwari,  Nicholas DaSilva,  Kellen T McCaffrey,  Yousef A Beni,  Antonio González-Sarrías,  Navindra P Seeram,  Keykavous Parang,  Anil Kumar
Affiliations

Affiliation

  • 1 Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, Rajasthan, India.
PMID: 23953195 DOI: 10.1016/j.bmcl.2013.07.058
Abstract

Simple and efficient synthesis of quebecol and a number of its analogs was accomplished in five steps. The synthesized compounds were evaluated for antiproliferative activities against human cervix adenocarcinoma (HeLa), human ovarian carcinoma (SK-OV-3), human colon carcinoma (HT-29), and human breast adenocarcinoma (MCF-7) Cancer cell lines. Among all the compounds, 7c, 7d, 7f, and 8f exhibited antiproliferative activities against four tested cell lines with inhibition over 80% at 75 μM after 72 h, whereas, compound 7b and 7g were more selective towards MCF-7 cell line. The IC50 values for compounds 7c, 7d, and 7f were 85.1 μM, 78.7 μM, and 80.6 μM against MCF-7 cell line, respectively, showing slightly higher antiproliferative activtiy than the synthesized and isolated quebecol with an IC50 value of 104.2 μM against MCF-7.

Keywords

Antiproliferative; Phenolic; Quebecol; Structure–activity relationship; Synthesis.

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