Issue 56, 2019
From the journal:

RSC Advances

A minimal structural variation can overcome tumour resistance of oxaliplatin: the case of 4,5-dehydrogenation of the cyclohexane ring†

Paride Papadia, ORCID logo ‡*ab   Valentina Gandin,‡c   Alessandra Barbanente,bd   Alessandro G. Ruello,bd   Cristina Marzano,c   Katia Micoli,bd   James D. Hoeschele,e   Giovanni Natilebd  and  Nicola Margiotta ORCID logo *bd  

* Corresponding authors

a Department of Biological and Environmental Sciences and Technologies (DiSTeBA), University of Salento, Prov.le Lecce-Monteroni, Centro Ecotekne, 73100 Lecce, Italy
E-mail: paride.papadia@unisalento.it
Tel: +39 832 299263

b CIRCMSB, Consorzio Interuniversitario di Ricerca in Chimica dei Metalli nei Sistemi Biologici, Via Celso Ulpiani 27, 70121 Bari, Italy

c Dipartimento di Scienze del Farmaco, Università di Padova, Via Marzolo 5, Padova, Italy

d Dipartimento di Chimica, Università degli Studi di Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy
E-mail: nicola.margiotta@uniba.it
Tel: +39 80 5442759

e Department of Chemistry, Eastern Michigan University, 48197 Ypsilanti, MI, USA

Abstract

A new family of anticancer compounds has been derived from oxaliplatin by inserting a double-bond between carbons 4 and 5 of the 1,2-diaminocyclohexane ring. Testing against a panel of human tumour cell lines including cervical (A431), ovarian (2008), and colon carcinomas (HCT-15 and LoVo), and two oxaliplatin-resistant clones (LoVo OXP and LoVo MDR) has shown that the new compounds have, in general, equal if not better cytotoxic activity and are able to overcome the oxaliplatin-resistance. Moreover, the oxalato derivative induced lipid droplets increase in LoVo OXP cells thus suggesting the involvement of metabolism stress in its mechanism of action.

Graphical abstract: A minimal structural variation can overcome tumour resistance of oxaliplatin: the case of 4,5-dehydrogenation of the cyclohexane ring

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Article information

DOI
https://doi.org/10.1039/C9RA07760J
Article type
Paper
Submitted
24 Sep 2019
Accepted
30 Sep 2019
First published
11 Oct 2019
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2019,9, 32448-32452

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A minimal structural variation can overcome tumour resistance of oxaliplatin: the case of 4,5-dehydrogenation of the cyclohexane ring

P. Papadia, V. Gandin, A. Barbanente, A. G. Ruello, C. Marzano, K. Micoli, J. D. Hoeschele, G. Natile and N. Margiotta, RSC Adv., 2019, 9, 32448 DOI: 10.1039/C9RA07760J

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