Herein, we report on the synthesis and the evaluation of preliminary antitumor properties of a small collection of platinum(II) complexes in which a cisplatin-like unit is tethered to 7- deazaadenosine through linear alkyl chains (from 1 to 6 carbon atoms) installed at the purine C6-position. The complexation is performed by exploiting the reactivity of the bidentate amino ligands (R)- and (S)-2,3-diaminopropanoic acids (DAPA) attached at the end of the alkyl chain spacer. By varying the length of the alkyl chain and the chirality of the DAPA moiety we obtained ten novel nucleoside- platinum complexes, whose anti-cancer properties have been evaluated against the A549 and Cal27 human cancer cell lines.

Synthesis and Evaluation of the Antitumor Properties of a Small Collection of Pt(II) Complexes with 7-Deazaadenosine as Scaffold / D'Errico, Stefano; Borbone, Nicola; Piccialli, Vincenzo; Di Gennaro, Elena; Zotti, Andrea; Budillon, Alfredo; Vitagliano, Carlo; Piccialli, Ilaria; Oliviero, Giorgia. - In: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY. - ISSN 1434-193X. - 2017:33(2017), pp. 4935-4947. [10.1002/ejoc.201700730]

Synthesis and Evaluation of the Antitumor Properties of a Small Collection of Pt(II) Complexes with 7-Deazaadenosine as Scaffold

D'ERRICO, STEFANO;BORBONE, NICOLA;PICCIALLI, VINCENZO;BUDILLON, Alfredo;VITAGLIANO, CARLO;PICCIALLI, ILARIA;OLIVIERO, GIORGIA
2017

Abstract

Herein, we report on the synthesis and the evaluation of preliminary antitumor properties of a small collection of platinum(II) complexes in which a cisplatin-like unit is tethered to 7- deazaadenosine through linear alkyl chains (from 1 to 6 carbon atoms) installed at the purine C6-position. The complexation is performed by exploiting the reactivity of the bidentate amino ligands (R)- and (S)-2,3-diaminopropanoic acids (DAPA) attached at the end of the alkyl chain spacer. By varying the length of the alkyl chain and the chirality of the DAPA moiety we obtained ten novel nucleoside- platinum complexes, whose anti-cancer properties have been evaluated against the A549 and Cal27 human cancer cell lines.
2017
Synthesis and Evaluation of the Antitumor Properties of a Small Collection of Pt(II) Complexes with 7-Deazaadenosine as Scaffold / D'Errico, Stefano; Borbone, Nicola; Piccialli, Vincenzo; Di Gennaro, Elena; Zotti, Andrea; Budillon, Alfredo; Vitagliano, Carlo; Piccialli, Ilaria; Oliviero, Giorgia. - In: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY. - ISSN 1434-193X. - 2017:33(2017), pp. 4935-4947. [10.1002/ejoc.201700730]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/681087
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