A review on anticancer potential of bioactive heterocycle quinoline

Afzal, Obaid; Kumar, Suresh; Haider, Rafi; Ali, Rahmat; Kumar, Rajiv; Jaggi, Manu; Bawa, Sandhya

doi:10.1016/j.ejmech.2014.07.044

Cited by 678 publications

(296 citation statements)

References 256 publications

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“…Owing to its ability to bind copper/zinc and dissolve beta-amyloid plaques by activating autophagy in the brain, clioquinol has re-emerged as a potential therapy for Alzheimer's disease (6,7). Clioquinol was also reported to have anticancer activity in several carcinoma cells (8)(9)(10)(11). Especially, in preclinical models of hematologic malignancies and solid tumors, clioquinol displays anticancer efficacy in vitro and in vivo (12)(13)(14).…”

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confidence: 99%

Induction of cell cycle arrest via the p21, p27–cyclin E,A/Cdk2 pathway in SMMC-7721 hepatoma cells by clioquinol

et al. 2015

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Induction of cell cycle arrest via the p21, p27-cyclin E,A/Cdk2 pathway in SMMC-7721 hepatoma cells by clioquinolClioquinol has been shown to have anticancer activity in several carcinoma cells. In this study, we preliminarily examined the effect of clioquinol in human SMMC-7721 hepatoma and QSG-7701 normal hepatic cells. Our results indicated that clioquinol did not significantly affect survival of QSG-7701 cells, whereas it reduced cell viability in a concentration-and time-dependent manner in SMMC-7721 cells. Clioquinol did not trigger autophagy and apoptosis, while it induced cell cycle arrest in the S-phase in SMMC-7721 cells. Additionally, down-regulation of cyclin D1, A2, E1, Cdk2 and up-regulation of p21, p27 were detected after the treatment with clioquinol. The results demonstrated for the first time that clioquinol suppressed cell cycle progression in the S-phase in SMMC-7721 cells via the p21, p27-cyclin E,A/Cdk2 pathway. This suggests that clioquinol may have a therapeutic potential as an anticancer drug for certain malignances.

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Induction of cell cycle arrest via the p21, p27–cyclin E,A/Cdk2 pathway in SMMC-7721 hepatoma cells by clioquinol

et al. 2015

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“…These pharmacological activities include DNA binding 4 , antitumor [5][6][7] , benzodiazepine and GABA receptor ligand activity 8 , antiviral 9,10 , antibacterial 11 , antituberculosis 12,13 and cellular phosphorylation and tyrosine kinase inhibition 14 . Many marketed drugs comprise quinazoline nucleus in their structures such as; , treatment of lupus 25 , treatment of neurodegenerative diseases 26 , antitubercular 27,28 , antiprotozoal 29,30 and anticancer 31,32 . Among the marketed drugs carrying quinoline nucleus is the fluoroquinolone antibacterial ciprofloxacin.…”

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confidence: 99%

Synthesis and Antimicrobial Evaluation of Some Tricyclic Substituted benzo[h]quinazolines, benzo[h]quinolines and naphthaleno[d]thiazoles

Ebied

Zaghary

Amin

et al. 2017

Journal of Advanced Pharmacy Research

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Objectives: The notable advancing in the medicinal chemistry arena against infectious diseases has resulted in the discovery of numerous valuable antimicrobial drugs that saved millions of lives throughout the last few decades. Nevertheless, the continuous reporting of multi-drug resistant strains of a number of diverse germs makes the need for novel broad-spectrum anti-infective agents still exists. Methods: Three series of ring-equivalent tricyclic benzo The antimicrobial activity of some of the synthesized compounds was screened and only 2-bromo derivative IX and aminothiazole compound X exhibited broad antimicrobial effectiveness. The antifungal MIC value of X was1.85 mg/mL. Conclusion:The new synthesized compounds, designed as bioisosteres, showed excellent potency against the tested gram (+) bacterial and fungal strains compared to reference drugs.

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“…The natural compounds containing the quinolin-2-one nucleus such as flindersine, dictamnine as well as their synthetic analogues are found to possess pharmacological activity and therapeutic utility [2][3][4][5]. Clinical significance of quinolin-2-one is well established and documented in the form of treatment of psychosis, as a β-blocker in an ophthalmic preparation, as an antacid and in congestive cardiac failure [6][7][8][9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Evaluation of 4-Hydroxy-1-Phenyl/Methyl-3-(3-Substituted-1-(Substitutedimino) Propyl) Quinoline-2(1h)-One Derivatives and 4-Hydroxy-1-Phenyl/Methyl-3-(1-(Substituedimino) Ethyl) Quinoline-2(1h)-One Derivatives as Possible Anticancer Agents

Desai¹,

Priolkar²,

Karmali³

et al. 2017

Int J Pharm Pharm Sci

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Objective: Synthesis, characterization and evaluation of quinolin-2-one derivatives as possible anticancer agents. Methods:A series of novel 4-hydroxy-1-phenyl/methyl-3-(3-substituted-1-(substitutedimino)propyl)quinolin-2(1H)-one derivatives IIa(1-5)/IIb(1-5) and 4-hydroxy-1-phenyl/methyl-3-(1-(substituedimino)ethyl)quinolin-2(1H)-one derivatives IIIa(1-3)/IIIb(1-3) were synthesised by nucleophilic addition of substituted anilines on 3-acetyl-4-hydroxy-1-phenyl/methylquinolin-2(1H)-one (a/b) and 4-hydroxy-3-(3-substitutedpropanoyl)-1-phenyl/methyl quinolin-2(1H)-one (Ia/Ib); respectively. The synthesised derivatives were characterised by spectral analysis and were tested for their in vitro anticancer activity against K562 and Hep 3b cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method.Results: The compounds were tested for their in vitro anticancer activity against K562 and Hep 3b cell lines at 10, 20, 25, 30 and 50 µg/ml concentration using MTT assay method. The compound 4-hydroxy-3-(3-morpholino-1-(phenylimino)propyl)-1-phenylquinolin-2(1H)-one (IIa-1) showed anticancer activity with IC50 value 20 µg as compared to the control against K562 cell lines. The compound 4-hydroxy-1-phenyl-3-(1-(phenylimino) ethyl) quinolin-2(1H)-one (IIIa-1) showed anticancer activity with IC50 value less than 10 µg. Conclusion:The proposed method for the synthesis of novel derivatives is convenient and gives a good yield. Some of the synthesised compounds showed promising anticancer activity against K562 and Hep 3b cell lines. Compound IIa-1 (R=-C6H5; R1= morpholine; R2= C6H5-NH-) exhibited most potent activity against K562 cell lines. Compound IIIa-1 (R=-C6H5; R3= C6H5-NH-) has been proved to be the most cytotoxic compound among the other derivatives against Hep 3b cell lines.

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A review on anticancer potential of bioactive heterocycle quinoline

Cited by 678 publications

References 256 publications

Induction of cell cycle arrest via the p21, p27–cyclin E,A/Cdk2 pathway in SMMC-7721 hepatoma cells by clioquinol

Induction of cell cycle arrest via the p21, p27–cyclin E,A/Cdk2 pathway in SMMC-7721 hepatoma cells by clioquinol

Synthesis and Antimicrobial Evaluation of Some Tricyclic Substituted benzo[h]quinazolines, benzo[h]quinolines and naphthaleno[d]thiazoles

Synthesis, Characterization and Evaluation of 4-Hydroxy-1-Phenyl/Methyl-3-(3-Substituted-1-(Substitutedimino) Propyl) Quinoline-2(1h)-One Derivatives and 4-Hydroxy-1-Phenyl/Methyl-3-(1-(Substituedimino) Ethyl) Quinoline-2(1h)-One Derivatives as Possible Anticancer Agents

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