Publication

Tuning the hydrophobicity of ruthenium(II)-arene (RAPTA) drugs to modify uptake, biomolecular interactions and efficacy

Paul Joseph Dyson, Claudine Scolaro, Christian Hartinger, Gianni Sava
2007
Journal Articles

Abstract

The antitumor activity of the organometallic ruthenium(II)-arene mixed phosphine complexes, [Ru(h6-p-cymene)Cl(PTA)(PPh3)]BF4 1b and [Ru(h6-C6H5CH2CH2OH)Cl(PTA)(PPh3)]BF4 2b (PTA = 1,3,5-triaza-7-phosphaadamantane), have been evaluated in vitro and compared to their RAPTA analogs, [Ru(h6-p-cymene)Cl2(PTA)] 1a and [Ru(h6-C6H5CH2CH2OH)Cl2(PTA)] 2a. The results show that the addn. of the PPh3 ligand to 2a increases the cytotoxicity towards the TS/A adenocarcinoma cancer cells, which correlates with increased uptake, but also increases cytotoxicity to non-tumorigenic HBL-100 cells, thus decreasing selectivity. The decrease in selectivity has been correlated to increased DNA interactions relative to proteins, demonstrated by reactivity of the compds. with a 14-mer oligonucleotide and the model proteins ubiquitin and cytochrome-c.

Official source

https://infoscience.epfl.ch/entities/publication/246a312b-ea47-4c8f-951d-c5ab8481833c

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Paul Joseph Dyson, Claudine Scolaro, Christian Hartinger, Gianni Sava
2007
Journal Articles

Abstract

Official source

https://infoscience.epfl.ch/entities/publication/246a312b-ea47-4c8f-951d-c5ab8481833c

About this result

Related concepts (22)

Adenocarcinoma

Adenocarcinoma (ˌædɪnoʊkɑːrsɪˈnoʊmə; plural adenocarcinomas or adenocarcinomata ˌædɪnoʊkɑːrsɪˈnoʊmətə; AC) is a type of cancerous tumor that can occur in several parts of the body. It is defined as neoplasia of epithelial tissue that has glandular origin, glandular characteristics, or both. Adenocarcinomas are part of the larger grouping of carcinomas, but are also sometimes called by more precise terms omitting the word, where these exist.

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Esophageal cancer is cancer arising from the esophagus—the food pipe that runs between the throat and the stomach. Symptoms often include difficulty in swallowing and weight loss. Other symptoms may include pain when swallowing, a hoarse voice, enlarged lymph nodes ("glands") around the collarbone, a dry cough, and possibly coughing up or vomiting blood. The two main sub-types of the disease are esophageal squamous-cell carcinoma (often abbreviated to ESCC), which is more common in the developing world, and esophageal adenocarcinoma (EAC), which is more common in the developed world.

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