Synthesis and biological evaluation of some 2-(3,5-dimethyl-1H-pyrazol-1-yl)-1-arylethanones: Antibacterial, DNA photocleavage, and anticancer activities

Kumar, Vinod; Kaur, Kiranjeet; Karelia, Deepkamal; Beniwal, Vikas; Gupta, Girish Kumar; Sharma, Arun; Gupta, A. K.

doi:10.1016/j.ejmech.2014.05.004

Cited by 48 publications

(23 citation statements)

References 36 publications

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“…In particular, designing of the compound having ability to cleave DNA is utmost important not only from the primary biological point of view but also in terms of photodynamic therapeutic approach to develop potent drugs [42]. The extracts which were found to be active in CT-DNA cleavage have been screened for their antiproliferative study.…”

Section: Discussionmentioning

confidence: 99%

Antiproliferative and Dna Cleavage Activity of Various Solvent Extracts of Acacia Farnesiana Linn. Pod

Manjulatha

2017

Asian J Pharm Clin Res

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Objective: Cancer has become the major disease by uncontrolled cell growth effecting large population on the globe. This study, deals with antiproliferative activity of different solvent extracts, viz., n-hexane (S 1 ), dichloromethane (DCM) (S 2 ), and methanol (S 3 ) of Acacia farnesiana pod on four cancer cell lines, viz., chronic myelogenous leukemia (K562), breast cancer (MCF-7), hepatocellular carcinoma (HePG2), colorectal adenocarcinoma (Colo 205), and DNA cleavage activity of the extracts on CT-DNA. Methods:The antiproliferative study was performed by MTT assay and DNA cleavage studies of the solvent extracts (S 1 , S 2 , and S 3 ) and its fractions (S 4 and S 5 ) was carried out by agarose gel electrophoresis method. Results:The antiproliferative activity results revealed that n-hexane extract (S 1 ) has showed activity against MCF-7 (21.70 %) cell line and methanol extract (S 3 ) against K562 (24.5%) and HePG2 (23.3%) cell lines. The DNA cleavage could be seen at every concentration tested by n-hexane (S 1 ), DCM (S 2 ), and methanol (S 3 ) extracts and significant cleavage was observed at concentrations of 25, 50, and 100 µg by fractions (S 4 ) and (S 5 ) of methanol extract. Conclusion:The results indicated that the extract of A. farnesiana pod (n-hexane and methanol) has antiproliferative properties and the DNA cleavage studies performed on CT-DNA was found that the extracts and its fractions showed significant activity at the concentrations tested.

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Section: Discussionmentioning

confidence: 99%

Antiproliferative and Dna Cleavage Activity of Various Solvent Extracts of Acacia Farnesiana Linn. Pod

Manjulatha

2017

Asian J Pharm Clin Res

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“…The synthesis and inhibitory activity against A549 lung cancer cell line of a series of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-1-arylethanones were described by Kumar et al [27]. [32].…”

Section: Discussionmentioning

confidence: 99%

Recent Reports on Pyrazole-Based Bioactive Compounds as Candidate for Anticancer Agents

Ardiansah

2017

Asian J Pharm Clin Res

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Pyrazole is a five-membered heterocyclic compound containing two nitrogen atoms. Due to its biological significance, design of novel pyrazole derivatives has become an interesting research area. We report the current progress in the development of anticancer agents containing pyrazole ring covering the time span of the past few years (2013)(2014)(2015)(2016). The presence of this nucleus is accompanied with some side chains, functional groups, or in combination with other nucleus such as thiazole, thiourea, glucosamine, naphthalimide, and benzofuran. Several biologically active pyrazoles synthesized by numerous researchers across the world are summarized in this paper.

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“…The loci present in DNA are involved in regulatory processes such as gene expression, gene transcription, mutagenesis and carcinogenesis [43] . In particular, designing of the compound having ability to cleave DNA is utmost important not only from the primary biological point of view but also in terms of photodynamic therapeutic approach to develop potent drugs [44] . The extracts, which were found to be active in DNA-cleavage assay, were further screened for antiproliferative study.…”

Section: Short Communicationsmentioning

confidence: 99%

Antiproliferative and DNA-cleaving Activities and Phytochemical Screening of Balanites roxburghiana Linn. Fruit Extracts

Shekhar¹,

Manjulatha²,

Satyanarayan³

et al. 2018

pharmaceutical-sciences

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The present investigation dealt with the antiproliferative, DNA-cleaving and preliminary phytochemical screening of n-hexane, dichloromethane and methanol extracts of Balanites roxburghiana Linn. The 3-(4,5-dimethylthiazole-2yl)-2,5-diphenyltetrazolium bromide assay was used to assess the antiproliferative activity against chronic myelogenous leukaemia, hepatocellular carcinoma, breast cancer, cervical cancer, colorectal adenocarcinoma and normal human kidney embryonic cell lines. Calf-thymus DNA-cleavage analysis was performed by agarose gel electrophoresis at various concentrations from 10 to 100 µg and preliminary phytochemical screening has been performed using standard procedure. The antiproliferative assay results of the extracts revealed that the n-hexane and dichloromethane extracts were more active compared to the methanol extract. The methanol extract showed 21.7 % activity against breast cancer cell lines only. n-Hexane extract (V 1 ) exhibited DNA cleavage at all concentrations, which could be due to binding to DNA. The dichloromethane extract (V 2 ) exhibited DNA cleavage at all concentrations but a very prominent low molecular weight DNA band formation could be observed with increasing concentration of the extract, With the methanol extract (V 3 ), the DNA cleavage increased with concentration of the sample. A partial cleavage could be found at 10 µg concentration under a UV transilluminator. The preliminary phytochemical screening revealed presence of flavonoids, steroids, tannins and saponins.

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Synthesis and biological evaluation of some 2-(3,5-dimethyl-1H-pyrazol-1-yl)-1-arylethanones: Antibacterial, DNA photocleavage, and anticancer activities

Cited by 48 publications

References 36 publications

Antiproliferative and Dna Cleavage Activity of Various Solvent Extracts of Acacia Farnesiana Linn. Pod

Antiproliferative and Dna Cleavage Activity of Various Solvent Extracts of Acacia Farnesiana Linn. Pod

Recent Reports on Pyrazole-Based Bioactive Compounds as Candidate for Anticancer Agents

Antiproliferative and DNA-cleaving Activities and Phytochemical Screening of Balanites roxburghiana Linn. Fruit Extracts

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