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

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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 breast carcinoma (MCF-7) cell line compared with reference drugs cisplatin and 5-flourouracil
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Fig4: The dose response curve showing the in vitro inhibitory activity of the tested compounds against breast carcinoma (MCF-7) cell line compared with reference drugs cisplatin and 5-flourouracil

Mentions: Interestingly, the results are represented in Table 3 and Fig. 3 showed that compound 4a was the most active against the liver carcinoma cell line (HepG2), showing more activity than the reference drugs with IC50 value of 4.8 μg/mL compared to 5-flourouracil with IC50 value of 4.9 μg/mL and cisplatin with IC50 value of 18.8 μg/mL. Compound 3c exhibited good antitumor activity against the liver carcinoma cell line (HepG2) showing almost the same activity as cisplatin followed by 4b, 4c, 3d and 3a, respectively. The tested compounds showed lower tendency to inhibit the breast carcinoma cells than those observed for liver carcinoma (Fig. 4). The order of activity against breast carcinoma cell line (MCF-7) was 4a, 3c, 4b, and 4c, respectively. Moreover, compounds 3a, 3d, 3e and 4d were less active among their analogues against the two tumor cell lines.Table 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 breast carcinoma (MCF-7) 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

Fig4: The dose response curve showing the in vitro inhibitory activity of the tested compounds against breast carcinoma (MCF-7) cell line compared with reference drugs cisplatin and 5-flourouracil
Mentions: Interestingly, the results are represented in Table 3 and Fig. 3 showed that compound 4a was the most active against the liver carcinoma cell line (HepG2), showing more activity than the reference drugs with IC50 value of 4.8 μg/mL compared to 5-flourouracil with IC50 value of 4.9 μg/mL and cisplatin with IC50 value of 18.8 μg/mL. Compound 3c exhibited good antitumor activity against the liver carcinoma cell line (HepG2) showing almost the same activity as cisplatin followed by 4b, 4c, 3d and 3a, respectively. The tested compounds showed lower tendency to inhibit the breast carcinoma cells than those observed for liver carcinoma (Fig. 4). The order of activity against breast carcinoma cell line (MCF-7) was 4a, 3c, 4b, and 4c, respectively. Moreover, compounds 3a, 3d, 3e and 4d were less active among their analogues against the two tumor cell lines.Table 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