- Synthesis and evaluation of the anticancer activity of [Pt(diimine)(N,N-dibutyl-N′-acylthiourea)]+complexes
-
Despite the concerted efforts to develop targeted cancer treatments, these therapies are plagued by the rapid development of resistance and serious adverse drug reactions. Based on the wide clinical use and successes of the platinum drugs like cisplatin and oxaliplatin, we investigated the synthesis and potential anticancer efficacy of alternative platinum complexes. A series of nine cationic square planar platinum(ii) complexes were synthesized and characterized and then evaluated for their anticancer activity. The complexes were of the type [Pt(diimine)(Ln-κO,S)]+where diimine is either 1,10-phenanthroline (phen), 5,6-dimethyl-1,10-phenanthroline (dmp) or dipyrido[3,2-f:2′,3′-h]quinoxaline (dpq) and Ln-κO,Srepresenting variousN,N-dibutyl-N′-acylthiourea ligands. The anticancer activity of the synthesised complexes was evaluated against two lung cancer cell lines (A549 and H1975) and a colorectal cancer cell line, HT-29. The 50% inhibitory concentrations (IC50) for the most cytotoxic compounds were determined and the mode of cell death evaluated. The structure-activity relationships indicated that complexes with the 5,6-dimethyl-1,10-phenanthroline variation of the diimine ligand were the most active against the cell lines tested, while the activity of complexes based on the acylthiourea ligand varied between the cell lines. IC50values for the three active platinum complexes were in the low micromolar range for the three cell lines and ranged between 0.68 μM and 2.28 μM. Changes to cell morphology indicate that the active platinum complexes induce cell death by both apoptosis and paraptosis. The complexes were able to induce the nuclear expression of the cyclin-dependent kinase inhibitor, p21, which is an indicator of DNA damage. The collective data indicate that these platinum complexes are valuable lead compounds for further analysis and cancer drug discovery.
- Harmse, Leonie,Kotzé, Izak A.,Magwaza, Rachael N.,Peega, Tebogo
-
p. 11742 - 11762
(2021/09/06)
-
- Palladium(II)/N,N-disubstituted-N′-acylthioureas complexes as anti-Mycobacterium tuberculosis and anti-Trypanosoma cruzi agents
-
The new complexes of Pd(II) with N,N-disubstituted-N′-acylthioureas:[(1) [Pd(dppf)(N,N-dimethyl-N′-benzoylthioureato-k2O,S)]PF6, (2) [Pd(dppf)(N,N-diethyl-N′-benzoylthioureato-k2O,S)]PF6, (3) [Pd(dppf)(N,N-dibut
- Plutín, Ana M.,Alvarez, Anislay,Mocelo, Raúl,Ramos, Raúl,Castellano, Eduardo E.,da Silva, Monize M.,Villarreal, Wilmer,Pavan, Fernando R.,Meira, Cássio Santana,Filho, José Sim?o Rodrigues,Moreira, Diogo Rodrigo M.,Soares, Milena Botelho P.,Batista, Alzir A.
-
-
- Anti-Mycobacterium tuberculosis activity of platinum(II)/N,N-disubstituted-N′-acyl thiourea complexes
-
Synthesis, characterization and anti-Mycobacterium tuberculosis assays of new platinum(II)/dppf/N,N-disubstituted-N′-acyl thiourea complexes with general formulae [Pt(dppf)(L)]PF6, [dppf = 1,1′-bis(diphenylphosphino)ferrocene; L = N,N-disubstit
- Plutín, Ana M.,Alvarez, Anislay,Mocelo, Raúl,Ramos, Raúl,Castellano, Eduardo E.,Da Silva, Monize M.,Colina-Vegas, Legna,Pavan, Fernando R.,Batista, Alzir A.
-
-
- Tris-chelate complexes of cobalt(III) with N-[di(alkyl/aryl)carbamothioyl] benzamide derivatives: Synthesis, crystallography and catalytic activity in TBHP oxidation of alcohols
-
New six coordinated tris-chelate cobalt(III) complexes of the type [Co(L)3] (1-4) {where HL = N-[di(alkyl/aryl)carbamothioyl]benzamide derivatives}were prepared from the reaction between CoCl2· 6H2O and N-[di(alkyl/aryl)carbamothioyl]benzamide in ethanol and characterized by elemental analysis and spectral data (UV/Vis, IR, 1H & 13C NMR). The molecular structure of a representative complex [Co(L1)3] (1) [where HL1 = N-(diisopropylcarbamothioyl)benzamide], was determined by single crystal X-ray diffraction method and reveals a distorted octahedral geometry and a facial configuration of S atoms around the Co(III) center. These complexes act as efficient catalysts for the oxidation of alcohols to their corresponding aldehydes or ketones in presence of tert-butyl hydroperoxide (TBHP) at 80°C.
- Gunasekaran,Jerome,Ng, Seik Weng,Tiekink, Edward R.T.,Karvembu
-
body text
p. 156 - 162
(2012/02/16)
-
- Synthesis, characterization, and catalytic applications of Ru(III) complexes containing N-[di(alkyl/aryl)carbamothioyl]benzamide derivatives and triphenylphosphine/triphenylarsine
-
Six coordinated ruthenium(III) complexes of the type [RuX2(L)(PPh3)2] or [RuX2(L)(AsPh3)2] {where L = N-[di(alkyl/aryl)carbamothioyl]benzamide derivatives, X = Cl or Br} have been prepared by the reaction between [RuX3(PPh3)3] or [RuX3(AsPh3)3] (where X = Cl or Br) and N-[di(alkyl/aryl)carbamothioyl]benzamide derivatives in toluene and characterized by elemental analysis, spectral data (electronic, IR and EPR) and magnetic moment studies. The complexes act as efficient catalysts for the oxidation of alcohols in presence of N-methylmorpholine-N-oxide as oxidant at room temperature.
- Gunasekaran,Karvembu
-
body text
p. 952 - 955
(2011/01/07)
-
- New Reagents to Decompose Copper Complexes of Amino Acids
-
The use of N,N-dialkyl-N'-(benzoyl)thioureas in ethanol is an effective method to decompose copper complexes of amino acids.The reaction gives optimal yields, and no racemisation is observed.Furthermore, the recovery of the thiourea derivatives is an important advantage of this method.
- Koenig, Karl-Heinz,Kaul, Lothar,Kuge, Martin,Schuster, Michael
-
p. 1115 - 1116
(2007/10/02)
-
