Synthesis and evaluation of the diarylthiourea analogs as novel anti-cancer agents

  • Bioorg Med Chem Lett. 2015 Mar 15;25(6):1301-5. doi: 10.1016/j.bmcl.2015.01.042.
Shengquan Liu  1 ,  Maggie C Louie  2 ,  Vanishree Rajagopalan  3 ,  Guangyan Zhou  4 ,  Esmeralda Ponce  5 ,  Tran Nguyen  3 ,  Linda Green  5
Affiliations
  • 1. College of Pharmacy, Touro University-California, Vallejo, CA 94592, USA. Electronic address: [email protected].
  • 2. College of Pharmacy, Touro University-California, Vallejo, CA 94592, USA; Department of Natural Science and Mathematics, Dominican University of California, San Rafael, CA 94901, USA.
  • 3. College of Pharmacy, Touro University-California, Vallejo, CA 94592, USA.
  • 4. Department of Basic Science, Touro University-California, Vallejo, CA 94592, USA.
  • 5. Department of Natural Science and Mathematics, Dominican University of California, San Rafael, CA 94901, USA.
PMID: 25701251 DOI: 10.1016/j.bmcl.2015.01.042
Abstract

Ten p-nitrodiarylthiourea analogs were designed, synthesized and evaluated in breast (MCF-7, T-47D, MDA-MB-453) and prostate (DU-145, PC-3, LNCaP) Cancer cell lines for their Anticancer activities. The majority of the compounds were able to inhibit the growth of these six Cancer cell lines at low micromolar concentrations. Compound 7 was found to be the most potent Anticancer agent in this series with GI50 values of 3.16μM for MCF-7, 2.53μM for T-47D, 4.77μM for MDA-MB-453 breast Cancer lines and 3.54μM for LNCaP prostate Cancer cell line. These GI50 values were comparable to the parent compound, SHetA2.

Keywords
Anticancer agents; Breast cancer; Diarylthiourea analogs; Prostate cancer; SHetA2.