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Novel ruthenium and palladium complexes as potential anticancer molecules on SCLC and NSCLC cell lines

Onur Tokgun, Duygu Elma Karakas, Semih Tan, Ege Rıza Karagür, Behcet İnal, Hakan Akca, Feyyaz Durap, Akın Baysal, and Murat Aydemir

Faculty of Medicine, Department of Medical Genetics, Pamukkale University, Denizli, Turkey

 

E-mail: otokgun@pau.edu.tr

Received: 1 October 2019  Accepted: 5 March 2020

Abstract:

Lung cancer is one of the major causes of cancer-related deaths in the world. Non-small-cell lung cancer (NSCLC) is the most common type of lung cancer, and small-cell lung cancer (SCLC) is the most aggressive subtype of lung cancer. Proper therapies for SCLC have not yet been developed. However, new molecules have been designed and big innovation in treating SCLC has been achieved. Platinum-based antitumor drugs like cisplatin and carboplatin have several disadvantages including side effects, cisplatin-resistant tumors and limited solubility in aqueous media. Thus, two novel chiral aminoalcohol-based bis(phosphinite) ligands containing (η6-p-cymene)-Ru(II)-phosphinite and bis(phosphinite)–Pd(II) complexes were synthesized and evaluated for anticancer activity. In this study, the results showed that complex 1 has the strongest cytotoxic effects on SCLC and NSCLC cell lines. On the other hand, cisplatin, ruthenium and palladium complexes are capable to induce apoptosis. Especially, complexes 1 and 2 can induce apoptosis for both SCLC and NSCLC. When compared to the qRT-PCR and TUNEL results, we obtained a significant correlation between apoptotic index and p21, Bax gene expressions. This work revealed the potential of the synthesized complexes as anticancer agents with cytotoxic and pro-apoptotic activity as leading compounds for further anticancer researches.

Keywords: SCLC; NSCLC; Phosphinite; Palladium; Ruthenium; p21; Bax

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-020-01129-x

 

Chemical Papers 74 (9) 2883–2892 (2020)

Monday, October 25, 2021

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