Seleno-warfare against cancer: decoding antitumor activity of novel acylselenoureas and se-acylisoselenoureas

Date

2024

Authors

Angulo-Elizari, Eduardo
Raza, Asif
Sharma, Arun K.
Sanmartín, Carmen
Plano, Daniel

Director

Publisher

MDPI
Acceso abierto / Sarbide irekia
Artículo / Artikulua
Versión publicada / Argitaratu den bertsioa

Project identifier

Impacto
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No disponible en Scopus

Abstract

Currently, cancer remains a global health problem. Despite the existence of several treatments, including chemotherapy, immunotherapy, and radiation therapy, the survival rate for most cancer patients, particularly those with metastasis, remains unsatisfactory. Thus, there is a continuous need to develop novel, effective therapies. In this work, 22 novel molecules containing selenium are reported, including seven Se-acylisoselenoureas synthesized from aliphatic carbodiimides as well as acylselenoureas with the same carbo- and heterocycles and aliphatic amines. After an initial screening at two doses (50 and 10 µM) in MDA-MB-231 (breast), HTB-54 (lung), DU-145 (prostate), and HCT-116 (colon) tumor cell lines, the ten most active compounds were identified. Additionally, these ten hits were also submitted to the DTP program of the NCI to study their cytotoxicity in a panel of 60 cancer cell lines. Compound 4 was identified as the most potent antiproliferative compound. The results obtained showed that compound 4 presented IC50 values lower than 10 µM in the cancer cell lines, although it was not the most selective one. Furthermore, compound 4 was found to inhibit cell growth and cause cell death by inducing apoptosis partially via ROS production. Overall, our results suggest that compound 4 could be a potential chemotherapeutic drug for different types of cancer.

Description

Keywords

Acylisoselenourea, Acylselenourea, Antiproliferative, Apoptosis, Cancer, Carbodiimide, Selenium, Synthesis

Department

Ciencias de la Salud / Osasun Zientziak

Faculty/School

Degree

Doctorate program

item.page.cita

Angulo-Elizari, E., Raza, A., Encío, I., Sharma, A. K., Sanmartín, C., Plano, D. (2024) Seleno-warfare against cancer: decoding antitumor activity of novel acylselenoureas and se-acylisoselenoureas. Pharmaceutics, 16(2), 1-14. https://doi.org/10.3390/pharmaceutics16020272.

item.page.rights

© 2024 by the authors. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.

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