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Synthesis, structure, and tuberculostatic activity of dimethyl benzoylcarbonohydrazonodithioates.

Gobis K, Foks H, Zwolska Z, Augustynowicz-Kopeć E, Główka ML, Olczak A, Sabisz M - Monatsh. Chem. (2011)

Bottom Line: New dimethyl benzoylcarbonohydrazonodithioates were obtained by CS2 addition to arylcarboxylic acid hydrazides and methylation of the formed adduct.The new derivatives were tested for their activity against Mycobacterium tuberculosis.Some compounds exhibited high activity toward sensitive and resistant strains.

View Article: PubMed Central - PubMed

Affiliation: Department of Organic Chemistry, Medical University of Gdansk, Gdansk, Poland.

ABSTRACT

Abstract: New dimethyl benzoylcarbonohydrazonodithioates were obtained by CS2 addition to arylcarboxylic acid hydrazides and methylation of the formed adduct. The new derivatives were tested for their activity against Mycobacterium tuberculosis. Some compounds exhibited high activity toward sensitive and resistant strains.

No MeSH data available.


Related in: MedlinePlus

Effect of compounds 5, 7, and 10 on A549 (a) and HCT116 human cell lines (b)
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Fig2: Effect of compounds 5, 7, and 10 on A549 (a) and HCT116 human cell lines (b)

Mentions: Compounds 5, 7, and 10, the most active toward M. tuberculosis strains, were tested for cytotoxicity against human non-small lung cancer cell line A549 and human colon cancer cell line HCT116. Both lines were maintained in RPMI1640 or McCoy’s 5A medium, respectively, supplemented with 10% fetal bovine serum, 2 mM l-glutamine, and antibiotics (100 units/cm3 of penicillin and 100 mg cm−3 of streptomycin) at 37 °C in a 5% CO2/air atmosphere [21]. Cells were screened routinely for mycoplasma by the PCR method with a Mycoplasma Plus PCR Primer Set (Stratagene, La Jolla, CA, USA) [22]. The cytotoxicity of the tested compounds was determined by the MTT viability assay with exponentially growing cells and continuous drug exposure (120 h). After drug treatment cells were exposed to the MTT, a tetrazolium salt, for 4 h at 37 °C, and the formation of formazan was measured by a VICTOR 3V microplate reader (Wallac Perkin). The concentrations required to inhibit cell growth by 50% compared to untreated controls were determined from the curves plotting survival as a function of dose using the SlideWrite program (Fig. 2). All values are means of at least two independent experiments, each done in duplicate (Table 4). Cisplatin (Cis-Pt) and doxotubicin (Dox) were used as control cytostatic drugs. IC50 values determined in the A549 cell line were 0.63 ± 0.018 μM (Cis-Pt) and 0.008 ± 0.0011 μM (Dox).Fig. 2


Synthesis, structure, and tuberculostatic activity of dimethyl benzoylcarbonohydrazonodithioates.

Gobis K, Foks H, Zwolska Z, Augustynowicz-Kopeć E, Główka ML, Olczak A, Sabisz M - Monatsh. Chem. (2011)

Effect of compounds 5, 7, and 10 on A549 (a) and HCT116 human cell lines (b)
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4494766&req=5

Fig2: Effect of compounds 5, 7, and 10 on A549 (a) and HCT116 human cell lines (b)
Mentions: Compounds 5, 7, and 10, the most active toward M. tuberculosis strains, were tested for cytotoxicity against human non-small lung cancer cell line A549 and human colon cancer cell line HCT116. Both lines were maintained in RPMI1640 or McCoy’s 5A medium, respectively, supplemented with 10% fetal bovine serum, 2 mM l-glutamine, and antibiotics (100 units/cm3 of penicillin and 100 mg cm−3 of streptomycin) at 37 °C in a 5% CO2/air atmosphere [21]. Cells were screened routinely for mycoplasma by the PCR method with a Mycoplasma Plus PCR Primer Set (Stratagene, La Jolla, CA, USA) [22]. The cytotoxicity of the tested compounds was determined by the MTT viability assay with exponentially growing cells and continuous drug exposure (120 h). After drug treatment cells were exposed to the MTT, a tetrazolium salt, for 4 h at 37 °C, and the formation of formazan was measured by a VICTOR 3V microplate reader (Wallac Perkin). The concentrations required to inhibit cell growth by 50% compared to untreated controls were determined from the curves plotting survival as a function of dose using the SlideWrite program (Fig. 2). All values are means of at least two independent experiments, each done in duplicate (Table 4). Cisplatin (Cis-Pt) and doxotubicin (Dox) were used as control cytostatic drugs. IC50 values determined in the A549 cell line were 0.63 ± 0.018 μM (Cis-Pt) and 0.008 ± 0.0011 μM (Dox).Fig. 2

Bottom Line: New dimethyl benzoylcarbonohydrazonodithioates were obtained by CS2 addition to arylcarboxylic acid hydrazides and methylation of the formed adduct.The new derivatives were tested for their activity against Mycobacterium tuberculosis.Some compounds exhibited high activity toward sensitive and resistant strains.

View Article: PubMed Central - PubMed

Affiliation: Department of Organic Chemistry, Medical University of Gdansk, Gdansk, Poland.

ABSTRACT

Abstract: New dimethyl benzoylcarbonohydrazonodithioates were obtained by CS2 addition to arylcarboxylic acid hydrazides and methylation of the formed adduct. The new derivatives were tested for their activity against Mycobacterium tuberculosis. Some compounds exhibited high activity toward sensitive and resistant strains.

No MeSH data available.


Related in: MedlinePlus