2. Academic Validation
  3. Novel seleno- and thio-urea derivatives with potent in vitro activities against several cancer cell lines

Novel seleno- and thio-urea derivatives with potent in vitro activities against several cancer cell lines

  • Eur J Med Chem. 2016 May 4:113:134-44. doi: 10.1016/j.ejmech.2016.02.042.
Verónica Alcolea 1,  Daniel Plano 1,  Deepkamal N Karelia 2,  Juan Antonio Palop 3,  Shantu Amin 2,  Carmen Sanmartín 3,  Arun K Sharma 4
Affiliations

Affiliations

  • 1 Department of Pharmacology, Penn State Hershey Cancer Institute, CH72, Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, USA; Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea 1, E-31008 Pamplona, Spain; Instituto de Investigación Sanitaria de Navarra (IdiSNA), Irunlarrea 3, E-31008 Pamplona, Spain.
  • 2 Department of Pharmacology, Penn State Hershey Cancer Institute, CH72, Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, USA.
  • 3 Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea 1, E-31008 Pamplona, Spain; Instituto de Investigación Sanitaria de Navarra (IdiSNA), Irunlarrea 3, E-31008 Pamplona, Spain.
  • 4 Department of Pharmacology, Penn State Hershey Cancer Institute, CH72, Penn State College of Medicine, 500 University Drive, Hershey, PA 17033, USA. Electronic address: aks14@psu.edu.
PMID: 26922233 DOI: 10.1016/j.ejmech.2016.02.042
Abstract

A series of novel selenourea derivatives and corresponding thiourea analogs were synthesized and tested against a panel of six human Cancer cell lines: melanoma (1205Lu), lung carcinoma (A549), prostatic carcinoma (DU145), colorectal carcinoma (HCT116), pancreatic epithelioid carcinoma (PANC-1) and pancreatic adenocarcinoma (BxPC3). In general, we found that the selenium-containing derivatives were more potent than their isosteric sulfur analogs. Four selenourea derivatives (1e, 1f, 1g and 1i) showed IC50 values below 10 μM in all of tested cell lines at 72 h. On the basis of its potent activity, compound 1g was selected for further biological evaluation in different colon Cancer cell lines. Our results indicated that compound 1g induced Apoptosis by Caspase activation, along with inhibition of anti-apoptotic proteins.

Keywords

Apoptosis; Cytotoxicity; Selenium; Selenourea.

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