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3. Effect of chirality on the anticancer activity of Pt(ii) and Pt(iv) complexes containing 1R,2Rand 1S,2Senantiomers of thetrans-1,2-diamino-4-cyclohexene ligand (DACHEX), an analogue of diaminocyclohexane used in oxaliplatin

Author

Papadia, P., Barbanente, A., Ditaranto, N., Hoeschele, J. D., Natile, G., Marzano, C., Gandin, V., Margiotta, N., Papadia, P., Barbanente, A., Ditaranto, N., Hoeschele, J. D., Natile, G., Marzano, C., Gandin, V., and Margiotta, N.

Abstract

Six enantiomerically pure, oxaliplatin-like, platinum compounds (two platinum(ii) and four platinum(iv)), all containing unsaturated cyclic diaminetrans-1,2-diamino-4-cyclohexene (DACHEX) as a substitute for thetrans-1,2-diaminocyclohexane used in oxaliplatin, were investigated. The complexes were characterized by elemental analyses, ESI-MS, and1H-NMR spectroscopy. For the four Pt(iv) complexes the electrochemical redox behaviour, investigated by cyclic voltammetry, showed that all complexes possess reduction potentials suitable for activationin vivo. The antiproliferative activity was assessedin vitroon human cancer cell lines, also selected for resistance to platinum-based drugs or belonging to the MultiDrug-Resistant (MDR) phenotype. All complexes exhibited antiproliferative activity superior to that of cisplatin and almost equivalent to or better than that of oxaliplatin; moreover, most complexes were also capable of overcoming both the cisplatin- and the oxaliplatin-resistance. By comparing the effectiveness of the enantiomerically pure compounds with the racemic one, theR,Renantiomer emerged as the most effective in the case of Pt(ii) complexes whereas theS,Senantiomer was the most effective in the case of the Pt(iv) derivatives. From the results obtained also against 3D spheroid tumor models,cis,trans,cis-[Pt(OXA)(OBz)2(1S,2S-DACHEX)] (OBz = benzoate) emerged as the most promising candidate for further preclinical investigation.

Published
2021

8. A molecular tool for measuring the electron-acceptor ability of ligands from crystallographic data

Author

Fanizzi, F, Margiotta, N, Lanfranchi, M, Tiripicchio, A, Pacchioni, G, Natile, G, Natile, G., PACCHIONI, GIANFRANCO, Fanizzi, F, Margiotta, N, Lanfranchi, M, Tiripicchio, A, Pacchioni, G, Natile, G, Natile, G., and PACCHIONI, GIANFRANCO

Abstract

A method is proposed for the direct measurement of the pi-acidity of ligands coordinated to a metal center. The four-coordinate complex {[PtI2(Me-2-phen)] (Me-2-phen = 2,9-dimethyl-1,10-phenanthroline) is unique since it behaves as a molecular trap and, in the presence of a nucleophile (L), one end of it dissociates to allow the L ligand to coordinate trans to the monocoordinated diamine. The coordination of the free end of the phenanthroline is impeded by the filled d orbitals of the metal lying in the same plane as the phenanthrohne (d(yz) and d(z)(2) electrons assuming as x-axis that of the I-Pt-I vector). However, if the L ligand is a pi-acid able to remove electron charge from the yz plane, the second end of the phenanthroline will also be able to interact with platinum. A linear correlation is found between the crystallographic N-Pt-L angle 180degrees in ideal square-planar species and 143degrees in a trigonal bipyramid with a bite angle for bidentate Me-2-phen of 74degrees) and the pi-acceptor capacity of the L ligand as estimated by ab initio calculations. Alkenes and alkynes are found to be among the best pi-acids and lead to a regular trigonal-bipyramidal five-coordinate species. CO appears to be only halfway in between the best pi-acceptor ligands and those with smallest pi-acidity. P-, S-, and N-donor ligands follow in that order without significant differences between sulfides and sulfoxides or between aliphatic amines and pyridine. The very small difference between aliphatic amines and pyridine has been confirmed by investigation of the rate of exchange between the two ends for monocoordinated phenanthroline by H-1 NMR spectroscopy. The activation energy (DeltaG(double dagger)) was found to be equal, within the experimental error, for the two types of trans ligands

Published
2004

14. Cytotoxic Activity of [(R,R) and (S,S)-DACHPtCl(η2-C2H4)]Cl Complexes

Author

MIGONI, DANILO, BENEDETTI, MICHELE, CICCARESE, Antonella, FANIZZI, Francesco Paolo, MARSIGLIANTE, Santo, MARESCA L., NATILE G., Migoni, Danilo, Benedetti, Michele, Ciccarese, Antonella, Fanizzi, Francesco Paolo, Marsigliante, Santo, Maresca, L., and Natile, G.

Published
2004

28. Retro-modeling in Pt anticancer drug chemistry

Author

Marzilli L. G., Williams K., Sullivan S., Villanueva J., Ano SO, Marzilli P., Saad J., Intini F., Natile G., CICCARESE, Antonella, FANIZZI, Francesco Paolo, Marzilli, L. G., Williams, K., Sullivan, S., Villanueva, J., Ano, So, Marzilli, P., Saad, J., Ciccarese, Antonella, Intini, F., Fanizzi, Francesco Paolo, and Natile, G.

Published
1999

29. Reaction of Zn7metallothionein with cis- and trans-[Pt(N-donor)2Cl2] anticancer complexes: trans-Pt(II) complexes retain their N-donor ligands

Author

Knipp, M, Karotki, A V, Chesnov, S, Natile, G, Sadler, P J, Brabec, V, Vasák, M, University of Zurich, and Vasák, M

Subjects
1313 Molecular Medicine, 3002 Drug Discovery, 570 Life sciences, biology, 610 Medicine & health, 10071 Functional Genomics Center Zurich, U7 Systems Biology / Functional Genomics
Published
2007
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41. Unusual interstrand Pt(S,S-diaminocyclohexane)-GG crosslink formed by rearrangement of a classical intrastrand crosslink within a DNA duplex

Author

Cellular Protein Chemistry, Sub Cellular Protein Chemistry, Kubíček, K., Monnet, J., Scintilla, S., Kopečná, J., Arnesano, F., Trantirek, L., Chopard, C., Natile, G., Kozelka, J., Cellular Protein Chemistry, Sub Cellular Protein Chemistry, Kubíček, K., Monnet, J., Scintilla, S., Kopečná, J., Arnesano, F., Trantirek, L., Chopard, C., Natile, G., and Kozelka, J.

Published
2010

49. Cytotoxicity of some platinum(IV) complexes with ethylenediamine-N,N'-di-3-propionato ligand

Author

Sabo, Tibor, Kaluđerović, Goran N., Poleti, D, Karanovic, L, Boccarelli, A, Cannito, F, Natile, G, Sabo, Tibor, Kaluđerović, Goran N., Poleti, D, Karanovic, L, Boccarelli, A, Cannito, F, and Natile, G

Abstract

The cytotoxicities of two platinum(IV) complexes of formula [PtX(2)(eddp)] - nH(2)O (eddp = ethylenediamine-N,N'-di-3-propionate, X = chloro [11 or bromo [11], n = I or 1.24) are reported. The complexes have been obtained by direct reaction of potassium hexahaloplatinate(IV) with H(2)eddp.2HCl followed by addition of a base (LiOH). The crystal and molecular structure has confirmed that the complex with bromo ligands, similarly to the complex with chloro ligands previously reported, has trans configuration of the halogens. In both the chloro and bromo complexes there appear to be intramolecular N-H... X interactions which account for a narrowing of the corresponding X-Pt-N angles below 90degrees. The trans isomer (configuration index OC-6-13, two nitrogens and two oxygens of eddp bound in the equatorial plane) is the only one obtained in the reaction of hexahaloplatinate(IV) with the eddp ligand while a similar reaction performed with ethylenediamine-N,N'-diacetate (edda) affords exclusively the symmetrical cis-isomer (configuration index OC-6-33, equatorial nitrogen and axial oxygen atoms of edda). The longer chain of the propionato groups (as compared to the acetato ones) is responsible for such a change in preferred configuration. NMR data have revealed a very large diastereotopic splitting of the propionato methylene protons a to the nitrogens (0.88 ppm). The trans disposition of the halogen ligands in the compounds with eddp leads to deactivation of platinum(IV) complexes in comparison to those with edda having cis disposition of the leaving chlorides (human ovarian cancer cell line A2780, IC(50) [muM] of 92.6 +/- 12 and 30.3 +/- 7.5 for [1] and [11], respectively). (C) 2004 Elsevier Inc. All rights reserved.

Published
2004

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