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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

The interaction diagram showing hydrogen bonds and pi-pi interaction of (A) co-crystal ligand and (B) synthesized compound 10 with the active site of p38α MAP kinase
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Figure 5: The interaction diagram showing hydrogen bonds and pi-pi interaction of (A) co-crystal ligand and (B) synthesized compound 10 with the active site of p38α MAP kinase

Mentions: Figure 5 represents the interaction diagram showing hydrogen bonds and pi-pi interaction of (A) co-crystal ligand and (B-H) synthesized compounds (9-15) with the active site of the p38α MAP kinase. Compounds 9-13 and 15 interact with the p38α MAP kinase to form hydrogen bonds (green lines) with Asp-168 of p38MAPK. However, compound 14 interacts with the p38α MAP kinase to form a hydrogen bond with Met 109. Most of the synthesized compounds (9-11, 13, 15) show π-π interactions with Arg 67, and other residues like Lys 53 (9), His 148 (11), His 174 (13), Phe 169 (14). The binding affinity of synthetic compounds towards the active site of the p38α MAP kinase was in the order: 9 >10 > 12 > 15> 14> 13> 11.


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)

The interaction diagram showing hydrogen bonds and pi-pi interaction of (A) co-crystal ligand and (B) synthesized compound 10 with the active site of p38α MAP kinase
© Copyright Policy
Related In: Results  -  Collection

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

Figure 5: The interaction diagram showing hydrogen bonds and pi-pi interaction of (A) co-crystal ligand and (B) synthesized compound 10 with the active site of p38α MAP kinase
Mentions: Figure 5 represents the interaction diagram showing hydrogen bonds and pi-pi interaction of (A) co-crystal ligand and (B-H) synthesized compounds (9-15) with the active site of the p38α MAP kinase. Compounds 9-13 and 15 interact with the p38α MAP kinase to form hydrogen bonds (green lines) with Asp-168 of p38MAPK. However, compound 14 interacts with the p38α MAP kinase to form a hydrogen bond with Met 109. Most of the synthesized compounds (9-11, 13, 15) show π-π interactions with Arg 67, and other residues like Lys 53 (9), His 148 (11), His 174 (13), Phe 169 (14). The binding affinity of synthetic compounds towards the active site of the p38α MAP kinase was in the order: 9 >10 > 12 > 15> 14> 13> 11.

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