Gorakh S. Yellol
University of Murcia
Organic chemistryChemistryCisplatinBenzimidazoleLigand
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Publications 11
#1Enrique Ortega (University of Murcia)H-Index: 14
#2Jyoti G. Yellol (University of Murcia)H-Index: 5
Last. José Ruiz (University of Murcia)H-Index: 30
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A series of six osmium(II) complexes of the type [(η6-p-cymene)Os(C^N)X] (X = chlorido or acetato) containing benzimidazole C^N ligands with an ester group as a handle for further functionalization have been synthesized. They exhibit IC50 values in the low micromolar range in a panel of cisplatin (CDDP)-resistant cancer cells (approximately 10× more cytotoxic than CDDP in MCF-7), decrease the levels of intracellular ROS and reduce the NAD+ coenzyme, and inhibit tubulin polymerization. This disco...
2 CitationsSource
#1Vojtech NovohradskyH-Index: 12
#2Jyoti G. Yellol (University of Murcia)H-Index: 5
Last. Viktor BrabecH-Index: 53
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Our study demonstrates that four novel substitutionally inert C,N-cyclometalated Ru(II) complexes of the type [Ru(C^N)(N^N)2][PF6] containing a handle for functionalization in the C^N ligand are very potent cytotoxic agents against several different human cancer cell lines and are up to 400-fold more potent than clinically used cisplatin. In addition, the investigated ruthenium complexes are less cytotoxic in noncancerous cells, and exhibit higher selectivity for cancer cells than conventional p...
9 CitationsSource
#1Jyoti G. Yellol (University of Murcia)H-Index: 5
#2Sergio A. Pérez (University of Murcia)H-Index: 6
Last. José Ruiz (University of Murcia)H-Index: 30
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A series of 6 substitutionally inert and luminescent iridium(III) antitumor agents of the type [Ir(C∧N)2(N∧N)][PF6] containing a benzimidazole N∧N ligand with an ester group as a handle for further functionalization has been prepared. They exhibit IC50 values in the high nanomolar range in some ovarian and breast cancer cell lines (approximately 100× more cytotoxic than cisplatin (CDDP) in MDA-MB-231) and are located in the actin cortex predominantly as shown by confocal luminescence microscopy....
17 CitationsSource
#1Jyoti G. YellolH-Index: 5
#2Sergio A. PérezH-Index: 6
Last. José RuizH-Index: 30
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A series of novel C,N-cyclometalated benzimidazole ruthenium(II) and iridium(III) complexes of the types [(η6-p-cymene)RuCl(κ2-N,C-L)] and [(η5-C5Me5)IrCl(κ2-N,C-L)] (HL = methyl 1-butyl-2-arylbenzimidazolecarboxylate) with varying substituents (H, Me, F, CF3, MeO, NO2, and Ph) in the R4 position of the phenyl ring of 2-phenylbenzimidazole chelating ligand of the ruthenium (3a–g) and iridium complexes (4a–g) have been prepared. The cytotoxic activity of the new ruthenium(II) and iridium(III) com...
49 CitationsSource
#1Celina Støving Dam (UCPH: University of Copenhagen)H-Index: 2
#2Sergio Alejo Perez Henarejos (University of Murcia)H-Index: 1
Last. Stefan Stürup (UCPH: University of Copenhagen)H-Index: 26
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In the present work a novel C,N-cyclometalated benzimidazole Ru(II) arene complex (GY34) was characterized by applying an alternative, diverse approach considering both chemical and biological aspects. RP-HPLC-ICP-MS and RP-HPLC-ESI-MS analysis proved that GY34 in both RPMI-1640 cell medium and ammonium acetate buffer was transformed into several subspecies and the importance of evaluating and controlling analyte stability throughout experiments was demonstrated. Applying a novel cell fractionat...
7 CitationsSource
#1Ana ZamoraH-Index: 8
#2Sergio A. PérezH-Index: 6
Last. José RuizH-Index: 30
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A library of over 20 cycloplatinated compounds of the type [Pt(dmba-R)LCl] (dmba-R = C,N-dimethylbenzylamine-like ligand; R being MeO, Me, H, Br, F, CF3, and NO2 substituents in the R5 or R4 position of the phenyl ring; L = DMSO and P(C6H4CF3-p)3) has been prepared. All compounds are active in both human ovarian carcinoma A2780 cells and cisplatin-resistant A2780cisR cells, with most of the DMSO platinum complexes exhibiting IC50 values in the submicromolar range in the A2780 cell line. Interest...
31 CitationsSource
#1Gorakh S. YellolH-Index: 9
#2Jyoti G. YellolH-Index: 5
Last. José Rafael RuizH-Index: 32
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The design of small molecules that can target the aggregation of Aβ as potential therapeutic agents for Alzheimer’s disease is an area of study that has attracted a lot of attention recently. The novel ligand methyl 1-butyl-2-pyridyl-benzimidazole carboxylate was prepared for the synthesis of a series of new iridium(III), ruthenium(II), and platinum(II) 2-pyridyl-benzimidazole complexes. The crystal structure of the half-sandwich iridium(III) complex was established by X-ray diffraction. An arra...
28 CitationsSource
#1Natalia CutillasH-Index: 15
Last. José RuizH-Index: 30
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A series of potent C,N-cycloplatinated(II) phosphine antitumor complexes containing fluorous substituents in the cyclometalated or the ancillary phosphine ligands [Pt(C–N)(PR3)Cl] or both have been synthesized and characterized. The crystal structure of [Pt(dmba){P(C6H4CF3-p)3}Cl]·2CH2Cl2 (dmba = dimethylaminomethyl)phenyl) has been established by X-ray diffraction. Values of IC50 of the new platinum complexes were calculated toward a panel of human tumor cell lines representative of ovarian (A2...
21 CitationsSource
#1Gorakh S. Yellol (University of Murcia)H-Index: 9
#2Antonio Donaire (University of Murcia)H-Index: 18
Last. José Ruiz (University of Murcia)H-Index: 30
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Smart design and efficient synthesis of benzimidazole Ru, Ir and Rh cyclometalated complexes are reported with promising cytotoxic activity against HT29, T47D, A2780 and A2780cisR cancer cell lines. Their apoptosis, accumulation, cell cycle arrest, protein binding and DNA binding effects are also discussed.
52 CitationsSource
#1Ana Zamora (University of Murcia)H-Index: 8
#2Venancio Rodríguez (University of Murcia)H-Index: 19
Last. José Ruiz (University of Murcia)H-Index: 30
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Abstract Two new steroidal 7-azaindole-based N-donor ligands 17-α-[7-azaindole-5-ethynyl]-17-β-testosterone (ET-Haza) (1) and 17-α-[7-azaindole-5-ethynyl]-19-nortestosterone (LEV-Haza) (2), and two new DNA damaging warheads with an enhanced lipophilicity [Pt(dmba)Cl(L)] (dmba = N , N -dimethylbenzylamine-κN,κC; L = ET-Haza (3) and LEV-Haza (4)) have been prepared and characterized. Values of IC 50 were calculated for complexes 3 and 4 against a panel of human tumor cell lines representative of o...
16 CitationsSource