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

Verónica Alcolea, Daniel Plano, Deepkamal N. Karelia, Juan Antonio Palop, Shantu Amin, Carmen Sanmartín, Arun Sharma

Research output: Contribution to journalArticle

17 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)134-144
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume113
DOIs
StatePublished - May 4 2016

Fingerprint

Urea
Cells
Derivatives
Cell Line
Carcinoma
Neoplasms
Thiourea
Apoptosis Regulatory Proteins
Selenium
Caspases
Sulfur
Colonic Neoplasms
Inhibitory Concentration 50
Colorectal Neoplasms
Melanoma
Adenocarcinoma
Chemical activation
Apoptosis
Lung
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

Alcolea, Verónica ; Plano, Daniel ; Karelia, Deepkamal N. ; Palop, Juan Antonio ; Amin, Shantu ; Sanmartín, Carmen ; Sharma, Arun. / Novel seleno- and thio-urea derivatives with potent in vitro activities against several cancer cell lines. In: European Journal of Medicinal Chemistry. 2016 ; Vol. 113. pp. 134-144.
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Novel seleno- and thio-urea derivatives with potent in vitro activities against several cancer cell lines. / Alcolea, Verónica; Plano, Daniel; Karelia, Deepkamal N.; Palop, Juan Antonio; Amin, Shantu; Sanmartín, Carmen; Sharma, Arun.

In: European Journal of Medicinal Chemistry, Vol. 113, 04.05.2016, p. 134-144.

Research output: Contribution to journalArticle

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