The development and the synthesis of cationic platinum(II) complexes were realized and their cytotoxic activity was tested on triple negative breast cancer MDA-MB-231 cell line and in two cell lines poorly responsive to cisplatin (DLD-1 and MCF-7). The complex 2c resulted the most potent cytotoxic agent in MDA-MB-231 (IC50=61.9 µM) and more effective than cisplatin on both DLD-1 (IC50=57.4 µM) and MCF-7 (IC50=79.9 µM) cell lines. 2c showed different cellular uptake and pharmacodynamic properties than cisplatin, interfering with the progression of the M phase of the cell cycle. Thus, 2c represents a lead compound of a new class of cytotoxic agents with promising antitumor activity.

In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety / I. Rimoldi, G. Facchetti, G. Lucchini, E. Castiglioni, S. Marchianò, N. Ferri. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 25:6(2017), pp. 1907-1913. [10.1016/j.bmc.2017.02.010]

In vitro anticancer activity evaluation of new cationic platinum(II) complexes based on imidazole moiety

I. Rimoldi
;
G. Facchetti
Secondo
;
G. Lucchini;E. Castiglioni;S. Marchianò
Penultimo
;
2017

Abstract

The development and the synthesis of cationic platinum(II) complexes were realized and their cytotoxic activity was tested on triple negative breast cancer MDA-MB-231 cell line and in two cell lines poorly responsive to cisplatin (DLD-1 and MCF-7). The complex 2c resulted the most potent cytotoxic agent in MDA-MB-231 (IC50=61.9 µM) and more effective than cisplatin on both DLD-1 (IC50=57.4 µM) and MCF-7 (IC50=79.9 µM) cell lines. 2c showed different cellular uptake and pharmacodynamic properties than cisplatin, interfering with the progression of the M phase of the cell cycle. Thus, 2c represents a lead compound of a new class of cytotoxic agents with promising antitumor activity.
triple negative breast cancer; cationic platinum complex; imidazole; p53 expression; cell cycle
Settore CHIM/03 - Chimica Generale e Inorganica
Settore BIO/14 - Farmacologia
Article (author)
File in questo prodotto:
File Dimensione Formato  
1-s2.0-S0968089616311543-main.pdf

accesso riservato

Tipologia: Publisher's version/PDF
Dimensione 1.04 MB
Formato Adobe PDF
1.04 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
Manuscript Rimoldi BMC_revised.pdf

accesso aperto

Tipologia: Post-print, accepted manuscript ecc. (versione accettata dall'editore)
Dimensione 502.82 kB
Formato Adobe PDF
502.82 kB Adobe PDF Visualizza/Apri
Manuscript Rimoldi BMC_iris.pdf

accesso aperto

Tipologia: Pre-print (manoscritto inviato all'editore)
Dimensione 412.13 kB
Formato Adobe PDF
412.13 kB Adobe PDF Visualizza/Apri
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/491233
Citazioni
  • ???jsp.display-item.citation.pmc??? 6
  • Scopus 26
  • ???jsp.display-item.citation.isi??? 24
social impact