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Antimicrobial and anticancer activity of some novel fluorinated thiourea derivatives carrying sulfonamide moieties: synthesis, biological evaluation and molecular docking

View Article: PubMed Central

ABSTRACT

Background: Various thiourea derivatives have been used as starting materials for compounds with better biological activities. Molecular modeling tools are used to explore their mechanism of action.

4a4c4d4a: A new series of thioureas were synthesized. Fluorinated pyridine derivative showed the highest antimicrobial activity (with MIC values ranged from 1.95 to 15.63 µg/mL). Interestingly, thiadiazole derivative and coumarin derivative exhibited selective antibacterial activities against Gram positive bacteria. Fluorinated pyridine derivative was the most active against HepG2 with IC50 value of 4.8 μg/mL. Molecular docking was performed on the active site of MK-2 with good results.

4a: Novel compounds were obtained with good anticancer and antibacterial activity especially fluorinated pyridine derivative and molecular docking study suggest good activity as mitogen activated protein kinase-2 inhibitor.

No MeSH data available.


Related in: MedlinePlus

The dose response curve showing the in vitro inhibitory activity of the tested compounds against liver carcinoma (HepG2) cell line compared with reference drugs cisplatin and 5-flourouracil
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Fig3: The dose response curve showing the in vitro inhibitory activity of the tested compounds against liver carcinoma (HepG2) cell line compared with reference drugs cisplatin and 5-flourouracil

Mentions: The in vitro growth inhibitory activity of the synthesized compounds was investigated in comparison with the well-known anticancer standard drugs (5-flourouracil and cisplatin) under the same conditions using colorimetric MTT assay. Data generated were used to plot a dose response curve of which the concentration of test compounds required to kill 50% of cell population (IC50) was determined (Fig. 3). The results revealed that all the tested compounds showed inhibitory activity to the tumor cell lines in a concentration dependent manner. Cytotoxic activity was expressed as the mean IC50 of three independent experiments.Fig. 3


Antimicrobial and anticancer activity of some novel fluorinated thiourea derivatives carrying sulfonamide moieties: synthesis, biological evaluation and molecular docking
The dose response curve showing the in vitro inhibitory activity of the tested compounds against liver carcinoma (HepG2) cell line compared with reference drugs cisplatin and 5-flourouracil
© Copyright Policy - OpenAccess
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC5383913&req=5

Fig3: The dose response curve showing the in vitro inhibitory activity of the tested compounds against liver carcinoma (HepG2) cell line compared with reference drugs cisplatin and 5-flourouracil
Mentions: The in vitro growth inhibitory activity of the synthesized compounds was investigated in comparison with the well-known anticancer standard drugs (5-flourouracil and cisplatin) under the same conditions using colorimetric MTT assay. Data generated were used to plot a dose response curve of which the concentration of test compounds required to kill 50% of cell population (IC50) was determined (Fig. 3). The results revealed that all the tested compounds showed inhibitory activity to the tumor cell lines in a concentration dependent manner. Cytotoxic activity was expressed as the mean IC50 of three independent experiments.Fig. 3

View Article: PubMed Central

ABSTRACT

Background: Various thiourea derivatives have been used as starting materials for compounds with better biological activities. Molecular modeling tools are used to explore their mechanism of action.

4a4c4d4a: A new series of thioureas were synthesized. Fluorinated pyridine derivative showed the highest antimicrobial activity (with MIC values ranged from 1.95 to 15.63 µg/mL). Interestingly, thiadiazole derivative and coumarin derivative exhibited selective antibacterial activities against Gram positive bacteria. Fluorinated pyridine derivative was the most active against HepG2 with IC50 value of 4.8 μg/mL. Molecular docking was performed on the active site of MK-2 with good results.

4a: Novel compounds were obtained with good anticancer and antibacterial activity especially fluorinated pyridine derivative and molecular docking study suggest good activity as mitogen activated protein kinase-2 inhibitor.

No MeSH data available.


Related in: MedlinePlus