In vitro and in vivo evaluation of isatin-β-thiosemicarbazone and marboran against vaccinia and cowpox virus infections

Quenelle, Debra C.; Keith, Kathy A.; Kern, Earl R.

doi:10.1016/j.antiviral.2006.02.010

Cited by 118 publications

(74 citation statements)

References 23 publications

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“…2 Specific feature of TSCs and their metal complexes is their broad spectrum of biological properties including antiviral, antibacterial, antimalarial, antifungal and anticancer activity. 3,4,5,6 α-Nheterocyclic TSCs (HCTs) are known for their anticancer activity since the 1950s when 2-formylpyridine thiosemicarbazone was discovered to possess in vivo antileukemic activity in a mice model. 7 The best studied HCT to date is 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP), also referred to as Triapine, which has already been examined in several clinical phase I and II trials.…”

Section: Introductionmentioning

confidence: 99%

Effects of Terminal Dimethylation and Metal Coordination of Proline-2-formylpyridine Thiosemicarbazone Hybrids on Lipophilicity, Antiproliferative Activity, and hR2 RNR Inhibition

et al. 2014

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The nickel(II), copper(II) and zinc(II) complexes of the proline-thiosemicarbazone hybrids 3-methyl-(S)-pyrrolidine-2-carboxylate-2-formylpyridine thiosemicarbazone (L-Pro-FTSC or (S)-H 2 L 1 ) and 3-methyl-(R)-pyrrolidine-2-carboxylate-2-formylpyridine thiosemicarbazonehave been synthesized and characterized by elemental analysis, one-and two-dimensional 1 H and 13 C NMR spectroscopy, CD, UV−vis and ESI mass spectrometry. Compounds 13, 6 and 7 have been also studied by single crystal X-ray diffraction. Magnetic properties and solid state high-field EPR spectra of 2 over the range 50420 GHz were investigated. The complex formation processes of L-Pro-FTSC with nickel(II) and zinc(II) have been studied in aqueous solution due to the excellent water solubility of the complexes via pH-potentiometry, UV−vis and 1 H NMR spectroscopy. The results of the antiproliferative activity in vitro showed that dimethylation improves the cytotoxicity and hR2 RNR inhibition. Therefore introduction of more lipophilic groups into thiosemicarbazone-proline backbone becomes an option for the synthesis of more efficient cytotoxic agents of this family of compounds.3

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Section: Introductionmentioning

confidence: 99%

Effects of Terminal Dimethylation and Metal Coordination of Proline-2-formylpyridine Thiosemicarbazone Hybrids on Lipophilicity, Antiproliferative Activity, and hR2 RNR Inhibition

et al. 2014

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“…Many heterocyclic thiosemicarbazone derivatives and their platinum and palladium complexes have a wide range of pharmacological activities, such as antituberculosis [28], antibacterial [29], antitumor [30], antiprotozoal [31], antimalarial [32], antimicrobial [33], antiviral [34], antifungal [35], anticonvulsant [36] and anti-trypanosomal [37] activities. In our present work, the synthesis and characterization of thiosemicarbazones derived from 5-substitutedthiophene-2-carboxaldehydes and their platinum(II) and palladium(II) complexes are reported.…”

Section: Introductionmentioning

confidence: 99%

Novel platinum(II) and palladium(II) complexes of thiosemicarbazones derived from 5-substitutedthiophene-2-carboxaldehydes and their antiviral and cytotoxic activities

Karaküçük‐İyidoğan

Tasdemir

Oruç‐Emre

et al. 2011

European Journal of Medicinal Chemistry

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a b s t r a c tA series of thiosemicarbazones and their platinum(II) and palladium(II) complexes have been synthesized. The chemical structures of ligands and their complexes were characterized by UVeVis, IR, 1 H NMR, 13 C NMR, MS spectra, elemental analysis and TGA. The antiviral and cytotoxic activities of all compounds have been tested. Results of broad antiviral evaluation showed that none of the compounds evaluated endowed with anti-DNA or -RNA virus activity at subtoxic concentrations except for the palladium complex 1b. This compound exhibited slightly selective inhibition against cytomegalovirus. The platinum complex 4a exhibited the best cytostatic activities against human cervix carcinoma. Ligands 2, 4 and 5 showed cytostatic potential. The palladium complexes were in general less cytostatic than the corresponding platinum complexes or unliganded congeners.

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“…Thiosemicarbazones and their deviatives have been the subject of extensive investigation primarily because of their biological activities, such as antitumor [1,2], antiviral [3], antibacterial [4], antimalarial [5], antifungal [6], anti-inflammatory [7] and anti-HIV activities [8] and remarkable coordination properties [9][10][11]. The title compound was obtained within our project of studying thiosemicarbazones coordination compounds as potential anti-HIV-1 drugs.…”

Section: Discussionmentioning

confidence: 99%

Crystal structure of 4-formylpyridine thiosemicarbazonium nitrate hydrate, [C7H9N4S][NO3] · H2O

Zhang¹

2009

Zeitschrift Für Kristallographie - New Crystal Structures

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Source of materialAll the chemicals used were of AR grade. Asolution of thiosemicarbazone (0.091 g, 1m mol) in methanol (5 ml) was added dropwise to as olution of pyridine-4-carbaldehyde (0.11 g, 1 mmol) in methanol (5 ml) at room temperature with stirring for 2.h. To the above solution was added Co(NO 3 ) 2 · 6H 2 O(0.291 g, 1mmol) in 10 ml methanol with stirring for 12 h. The mixture solution was filtered. After keeping the filtrate in air for 3days, pale yellow crystals were formed. Experimental detailsH8 and H9 were found from Four difference maps and refined, the other hydrogen atoms were positioned geometrically and refined using ar iding model, with d(C-H) =0 .85 -0 .97 Å and with U iso(H) =1.2 Ueq(C). Discussion

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In vitro and in vivo evaluation of isatin-β-thiosemicarbazone and marboran against vaccinia and cowpox virus infections

Cited by 118 publications

References 23 publications

Effects of Terminal Dimethylation and Metal Coordination of Proline-2-formylpyridine Thiosemicarbazone Hybrids on Lipophilicity, Antiproliferative Activity, and hR2 RNR Inhibition

Effects of Terminal Dimethylation and Metal Coordination of Proline-2-formylpyridine Thiosemicarbazone Hybrids on Lipophilicity, Antiproliferative Activity, and hR2 RNR Inhibition

Novel platinum(II) and palladium(II) complexes of thiosemicarbazones derived from 5-substitutedthiophene-2-carboxaldehydes and their antiviral and cytotoxic activities

Crystal structure of 4-formylpyridine thiosemicarbazonium nitrate hydrate, [C7H9N4S][NO3] · H2O

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