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

doi:10.1016/j.ejmech.2016.02.042

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 journal › Article › peer-review

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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 language	English (US)
Pages (from-to)	134-144
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	113
DOIs	https://doi.org/10.1016/j.ejmech.2016.02.042
State	Published - May 4 2016

All Science Journal Classification (ASJC) codes

Pharmacology
Drug Discovery
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ejmech.2016.02.042

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

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.",

author = "Ver{\'o}nica Alcolea and Daniel Plano and Karelia, {Deepkamal N.} and Palop, {Juan Antonio} and Shantu Amin and Carmen Sanmart{\'i}n and Arun Sharma",

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doi = "10.1016/j.ejmech.2016.02.042",

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T1 - Novel seleno- and thio-urea derivatives with potent in vitro activities against several cancer cell lines

AU - Alcolea, Verónica

AU - Plano, Daniel

AU - Karelia, Deepkamal N.

AU - Palop, Juan Antonio

AU - Amin, Shantu

AU - Sanmartín, Carmen

AU - Sharma, Arun

PY - 2016/5/4

Y1 - 2016/5/4

N2 - 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.

AB - 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.

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JO - European Journal of Medicinal Chemistry

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ER -

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

Abstract

All Science Journal Classification (ASJC) codes

UN SDGs

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