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Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma.
Eur J Med Chem. 2020 Jul 12; 204:112583.EJ

Abstract

Combination therapy targeting both tumor growth and vascularization is considered to be a cornerstone for colorectal carcinomas (CRC) treatment. However, the major obstacles of most clinical anticancer drugs are their weak selective activity towards cancer cells and inherent inner organs toxicity, accompanied with fast drug resistance development. In our effort to discover novel selective and non-toxic agents effective against CRC, we designed, synthesized and characterized a series of rhenium(I) tricarbonyl-based complexes with increased lipophilicity. Two of these novel compounds were discovered to possess remarkable anticancer, anti-angiogenic and antimetastatic activity in vivo (zebrafish-human HCT-116 xenograft model), being effective at very low doses (1-3 μM). At doses as high as 250 μM the complexes did not provoke toxicity issues encountered in clinical anticancer drugs (cardio-, hepato-, and myelotoxicity). In vivo assays showed that the two compounds exceed the anti-tumor and anti-angiogenic activity of clinical drugs cisplatin and sunitinib malate, and display a large therapeutic window.

Authors+Show Affiliations

Department of Chemistry, Fribourg University, Chemin Du Musée 9, 1700, Fribourg, Switzerland.Institute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11042 152, Belgrade, Republic of Serbia. Electronic address: sasapavic@imgge.bg.ac.rs.Department of Chemistry, Fribourg University, Chemin Du Musée 9, 1700, Fribourg, Switzerland.Institute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11042 152, Belgrade, Republic of Serbia.Department of Chemistry, Fribourg University, Chemin Du Musée 9, 1700, Fribourg, Switzerland.Institute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11042 152, Belgrade, Republic of Serbia. Electronic address: jasmina.nikodinovic@imgge.bg.ac.rs.Department of Chemistry, Fribourg University, Chemin Du Musée 9, 1700, Fribourg, Switzerland. Electronic address: fabio.zobi@unifr.ch.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32731186

Citation

Delasoie, Joachim, et al. "Identification of Novel Potent and Non-toxic Anticancer, Anti-angiogenic and Antimetastatic Rhenium Complexes Against Colorectal Carcinoma." European Journal of Medicinal Chemistry, vol. 204, 2020, p. 112583.
Delasoie J, Pavic A, Voutier N, et al. Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma. Eur J Med Chem. 2020;204:112583.
Delasoie, J., Pavic, A., Voutier, N., Vojnovic, S., Crochet, A., Nikodinovic-Runic, J., & Zobi, F. (2020). Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma. European Journal of Medicinal Chemistry, 204, 112583. https://doi.org/10.1016/j.ejmech.2020.112583
Delasoie J, et al. Identification of Novel Potent and Non-toxic Anticancer, Anti-angiogenic and Antimetastatic Rhenium Complexes Against Colorectal Carcinoma. Eur J Med Chem. 2020 Jul 12;204:112583. PubMed PMID: 32731186.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Identification of novel potent and non-toxic anticancer, anti-angiogenic and antimetastatic rhenium complexes against colorectal carcinoma. AU - Delasoie,Joachim, AU - Pavic,Aleksandar, AU - Voutier,Noémie, AU - Vojnovic,Sandra, AU - Crochet,Aurelien, AU - Nikodinovic-Runic,Jasmina, AU - Zobi,Fabio, Y1 - 2020/07/12/ PY - 2020/04/21/received PY - 2020/06/06/revised PY - 2020/06/14/accepted PY - 2020/7/31/pubmed PY - 2020/7/31/medline PY - 2020/7/31/entrez KW - Angiogenesis KW - Antimetastatic KW - Colorectal carcinoma KW - Rhenium KW - Xenograft KW - Zebrafish SP - 112583 EP - 112583 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 204 N2 - Combination therapy targeting both tumor growth and vascularization is considered to be a cornerstone for colorectal carcinomas (CRC) treatment. However, the major obstacles of most clinical anticancer drugs are their weak selective activity towards cancer cells and inherent inner organs toxicity, accompanied with fast drug resistance development. In our effort to discover novel selective and non-toxic agents effective against CRC, we designed, synthesized and characterized a series of rhenium(I) tricarbonyl-based complexes with increased lipophilicity. Two of these novel compounds were discovered to possess remarkable anticancer, anti-angiogenic and antimetastatic activity in vivo (zebrafish-human HCT-116 xenograft model), being effective at very low doses (1-3 μM). At doses as high as 250 μM the complexes did not provoke toxicity issues encountered in clinical anticancer drugs (cardio-, hepato-, and myelotoxicity). In vivo assays showed that the two compounds exceed the anti-tumor and anti-angiogenic activity of clinical drugs cisplatin and sunitinib malate, and display a large therapeutic window. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/32731186/Identification_of_novel_potent_and_non_toxic_anticancer_anti_angiogenic_and_antimetastatic_rhenium_complexes_against_colorectal_carcinoma_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(20)30555-9 DB - PRIME DP - Unbound Medicine ER -
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