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Cytotoxic and Antioxidant Activity of a Set of Hetero Bicylic Methylthiadiazole Hydrazones: A Structure-Activity Study.

Kodisundaram P, Duraikannu A, Balasankar T, Sundarao Ambure P, Roy K - Int J Mol Cell Med (2015)

Bottom Line: Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects.The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis.Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemistry, Annamalai University, Annamalai Nagar-608002, Tamilnadu, India.

ABSTRACT
The current study highlights the in vitro antioxidant and antitumor activity of the previously-synthesized hydrazone derivatives against various free radicals and human cancer cell lines, respectively. The anticancer efficacies of the compound were tested by measuring cytotoxicity in cancer cell lines HeLa, A549, and non-cancerous NL20 cells. Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects. The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis. The results from cytotoxicity and cell migration assay showed that the substitution of electron-withdrawing fluoro, chloro and bromo functional groups induced a significant (P< 0.001) loss of cell viability and inhibited the invasive potential of the human cancer cells. Additionally, these compounds showed significantly (P< 0.05) a less toxicity toward non-cancerous NL20 cells. Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

No MeSH data available.


Related in: MedlinePlus

Anti-invasive potential of synthetic compounds 10, 12 and 13 (8 μM) by cell migration assay. * Significantly different from untreated control cells (P<0.05
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Figure 4: Anti-invasive potential of synthetic compounds 10, 12 and 13 (8 μM) by cell migration assay. * Significantly different from untreated control cells (P<0.05

Mentions: The anti-invasive potential of synthetic compounds was examined by cell migration assay. Control cells have a stronger invasive potential as revealed by the increased number of cells (Figure 4 A and B). However, HeLa cells treated with compounds 10, 12 and 13 (8 μM) significantly (P< 0.001) mitigate the invasive potential of HeLa cells (Figure 4 A and B).


Cytotoxic and Antioxidant Activity of a Set of Hetero Bicylic Methylthiadiazole Hydrazones: A Structure-Activity Study.

Kodisundaram P, Duraikannu A, Balasankar T, Sundarao Ambure P, Roy K - Int J Mol Cell Med (2015)

Anti-invasive potential of synthetic compounds 10, 12 and 13 (8 μM) by cell migration assay. * Significantly different from untreated control cells (P<0.05
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4499575&req=5

Figure 4: Anti-invasive potential of synthetic compounds 10, 12 and 13 (8 μM) by cell migration assay. * Significantly different from untreated control cells (P<0.05
Mentions: The anti-invasive potential of synthetic compounds was examined by cell migration assay. Control cells have a stronger invasive potential as revealed by the increased number of cells (Figure 4 A and B). However, HeLa cells treated with compounds 10, 12 and 13 (8 μM) significantly (P< 0.001) mitigate the invasive potential of HeLa cells (Figure 4 A and B).

Bottom Line: Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects.The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis.Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemistry, Annamalai University, Annamalai Nagar-608002, Tamilnadu, India.

ABSTRACT
The current study highlights the in vitro antioxidant and antitumor activity of the previously-synthesized hydrazone derivatives against various free radicals and human cancer cell lines, respectively. The anticancer efficacies of the compound were tested by measuring cytotoxicity in cancer cell lines HeLa, A549, and non-cancerous NL20 cells. Compounds possessing electron-donor methoxy and methyl substitutions at the para position of the phenyl ring moiety showed a concentration dependent free radical scavenging effects. The free radical-scavenging potential of synthetic compounds 11 and 14 may have significant impact on the prevention of free radical-induced oxidative stress and carcinogenesis. The results from cytotoxicity and cell migration assay showed that the substitution of electron-withdrawing fluoro, chloro and bromo functional groups induced a significant (P< 0.001) loss of cell viability and inhibited the invasive potential of the human cancer cells. Additionally, these compounds showed significantly (P< 0.05) a less toxicity toward non-cancerous NL20 cells. Docking studies revealed interactions of compound 10 with p38α MAP kinase, which may be responsible of its anti-invasive and anti-proliferative effects.

No MeSH data available.


Related in: MedlinePlus