Potential anticancer heterometallic Fe-Au and Fe-Pd agents:Initial mechanistic insights

A series of gold(III) and palladium(II) heterometallic complexes with new iminophosphorane ligands derived from ferrocenylphosphanes [{Cp-P(Ph2)═N-Ph}2Fe] (1), [{Cp-P(Ph2)═N-CH2-2-NC5H4}2Fe] (2), and [{Cp-P(Ph2)═N-CH2-2-NC5H4}Fe(Cp)] (3) have been synthesized and structurally characterized. Ligands 2 and 3 afford stable coordination complexes [AuCl2(3)]ClO4, [{AuCl2}2(2)](ClO4)2, [PdCl2(3)], and [{PdCl2}2(2)]. The complexes have been evaluated for their antiproliferative properties in human ovarian cancer cells sensitive and resistant to cisplatin (A2780S/R), in human breast cancer cells (MCF7) and in a nontumorigenic human embryonic kidney cell line (HEK-293T). The highly cytotoxic trimetallic derivatives M2Fe (M = Au, Pd) are more cytotoxic to cancer cells than their corresponding monometallic fragments. Moreover, these complexes were significantly more cytotoxic than cisplatin in the resistant A2780R and the MCF7 cell lines. Studies of the interactions of the trimetallic compounds with DNA and the zinc-finger protein PARP-1 indicate that they exert anticancer effects in vitro based on different mechanisms of actions with respect to cisplatin

Luminescent iminophosphorane gold, palladium and platinum complexes as potential anticancer agents

A series of coordination gold(III), palladium(II), and platinum(II) complexes with a luminescent iminophosphorane ligand derived from 8-aminoquinoline [Ph3P[double bond, length as m-dash]N–C9H6N] (1) have been synthesized and structurally characterized. The coordination palladium(II) and platinum(II) compounds can evolve further, under appropriate conditions, to give stable cyclometalated endo species [M{κ3-C,N,N-C6H4(PPh2[double bond, length as m-dash]N-8-C9H6N)}Cl] (M = Pd, Pt) by C–H activation of the phenyl group of the PPh3 fragment. Iminophosphorane 1 and the new metallic complexes are luminescent in DMSO or DMSO–H2O (1 : 1 mixture) solutions at RT. The compounds have been evaluated for their antiproliferative properties in a human ovarian cancer cell line (A2780S), in human lung cancer cells (A549) and in a non-tumorigenic human embryonic kidney cell line (HEK-293T). Most compounds have been more toxic to the ovarian cancer cell line than to the non-tumorigenic cell line. The new complexes interact with human serum albumin (HSA) faster than cisplatin. Studies of the interactions of the compounds with DNA indicate that, in some cases, they exert anticancer effects in vitro based on different mechanisms of action with respect to cisplatin

Potential Anticancer Heterometallic Fe–Au and Fe–Pd Agents: Initial Mechanistic Insights

A series of gold­(III) and palladium­(II) heterometallic complexes with new iminophosphorane ligands derived from ferrocenylphosphanes [{Cp-P­(Ph₂)N-Ph}₂Fe] (<b>1</b>), [{Cp-P­(Ph₂)N-CH₂-2-NC₅H₄}₂Fe] (<b>2</b>), and [{Cp-P­(Ph₂)N-CH₂-2-NC₅H₄}­Fe­(Cp)] (<b>3</b>) have been synthesized and structurally characterized. Ligands <b>2</b> and <b>3</b> afford stable coordination complexes [AuCl₂(<b>3</b>)]­ClO₄, [{AuCl₂}₂(<b>2</b>)]­(ClO₄)₂, [PdCl₂(<b>3</b>)], and [{PdCl₂}₂(<b>2</b>)]. The complexes have been evaluated for their antiproliferative properties in human ovarian cancer cells sensitive and resistant to cisplatin (A2780S/R), in human breast cancer cells (MCF7) and in a nontumorigenic human embryonic kidney cell line (HEK-293T). The highly cytotoxic trimetallic derivatives M₂Fe (M = Au, Pd) are more cytotoxic to cancer cells than their corresponding monometallic fragments. Moreover, these complexes were significantly more cytotoxic than cisplatin in the resistant A2780R and the MCF7 cell lines. Studies of the interactions of the trimetallic compounds with DNA and the zinc-finger protein PARP-1 indicate that they exert anticancer effects in vitro based on different mechanisms of actions with respect to cisplatin

Potential Anticancer Heterometallic Fe–Au and Fe–Pd Agents: Initial Mechanistic Insights

A series of gold­(III) and palladium­(II) heterometallic complexes with new iminophosphorane ligands derived from ferrocenylphosphanes [{Cp-P­(Ph₂)N-Ph}₂Fe] (<b>1</b>), [{Cp-P­(Ph₂)N-CH₂-2-NC₅H₄}₂Fe] (<b>2</b>), and [{Cp-P­(Ph₂)N-CH₂-2-NC₅H₄}­Fe­(Cp)] (<b>3</b>) have been synthesized and structurally characterized. Ligands <b>2</b> and <b>3</b> afford stable coordination complexes [AuCl₂(<b>3</b>)]­ClO₄, [{AuCl₂}₂(<b>2</b>)]­(ClO₄)₂, [PdCl₂(<b>3</b>)], and [{PdCl₂}₂(<b>2</b>)]. The complexes have been evaluated for their antiproliferative properties in human ovarian cancer cells sensitive and resistant to cisplatin (A2780S/R), in human breast cancer cells (MCF7) and in a nontumorigenic human embryonic kidney cell line (HEK-293T). The highly cytotoxic trimetallic derivatives M₂Fe (M = Au, Pd) are more cytotoxic to cancer cells than their corresponding monometallic fragments. Moreover, these complexes were significantly more cytotoxic than cisplatin in the resistant A2780R and the MCF7 cell lines. Studies of the interactions of the trimetallic compounds with DNA and the zinc-finger protein PARP-1 indicate that they exert anticancer effects in vitro based on different mechanisms of actions with respect to cisplatin

Potential Anticancer Heterometallic Fe–Au and Fe–Pd Agents: Initial Mechanistic Insights

A series of gold­(III) and palladium­(II) heterometallic complexes with new iminophosphorane ligands derived from ferrocenylphosphanes [{Cp-P­(Ph₂)N-Ph}₂Fe] (<b>1</b>), [{Cp-P­(Ph₂)N-CH₂-2-NC₅H₄}₂Fe] (<b>2</b>), and [{Cp-P­(Ph₂)N-CH₂-2-NC₅H₄}­Fe­(Cp)] (<b>3</b>) have been synthesized and structurally characterized. Ligands <b>2</b> and <b>3</b> afford stable coordination complexes [AuCl₂(<b>3</b>)]­ClO₄, [{AuCl₂}₂(<b>2</b>)]­(ClO₄)₂, [PdCl₂(<b>3</b>)], and [{PdCl₂}₂(<b>2</b>)]. The complexes have been evaluated for their antiproliferative properties in human ovarian cancer cells sensitive and resistant to cisplatin (A2780S/R), in human breast cancer cells (MCF7) and in a nontumorigenic human embryonic kidney cell line (HEK-293T). The highly cytotoxic trimetallic derivatives M₂Fe (M = Au, Pd) are more cytotoxic to cancer cells than their corresponding monometallic fragments. Moreover, these complexes were significantly more cytotoxic than cisplatin in the resistant A2780R and the MCF7 cell lines. Studies of the interactions of the trimetallic compounds with DNA and the zinc-finger protein PARP-1 indicate that they exert anticancer effects in vitro based on different mechanisms of actions with respect to cisplatin

CCDC 977991: Experimental Crystal Structure Determination

Related Article: Malgorzata Frik, Josefina Jiménez, Vadim Vasilevski, Monica Carreira, Andreia de Almeida, Elena Gascón, Farrah Benoit, Mercedes Sanaú, Angela Casini, María Contel|2014|Inorg.Chem.Front.|1|231|doi:10.1039/C4QI00003J,An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

CCDC 930540: Experimental Crystal Structure Determination

Related Article: Nicholas Lease, Vadim Vasilevski, Monica Carreira, Andreia de Almeida, Mercedes Sanaú, Pipsa Hirva, Angela Casini, María Contel|2013|J.Med.Chem.|56|5806|doi:10.1021/jm4007615,An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

CCDC 977990: Experimental Crystal Structure Determination

Related Article: Malgorzata Frik, Josefina Jiménez, Vadim Vasilevski, Monica Carreira, Andreia de Almeida, Elena Gascón, Farrah Benoit, Mercedes Sanaú, Angela Casini, María Contel|2014|Inorg.Chem.Front.|1|231|doi:10.1039/C4QI00003J,An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

CCDC 930539: Experimental Crystal Structure Determination

Related Article: Nicholas Lease, Vadim Vasilevski, Monica Carreira, Andreia de Almeida, Mercedes Sanaú, Pipsa Hirva, Angela Casini, María Contel|2013|J.Med.Chem.|56|5806|doi:10.1021/jm4007615,An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.