Drug Design by Regression Analyses of Newly Synthesized Derivatives of 8-Quinolinol

Pavlov, Alexander; Takuchev, Nikolay; Georgieva, N.

doi:10.5504/50yrtimb.2011.0030

Cited by 4 publications

(3 citation statements)

References 11 publications

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“…Antimicrobial effects of 8HQ and its derivatives encompassing antibacterial,102–104 antimalarial,105–107 antiviral,108 antitubercular,109 and antidental plaque activities110,111 have been previously reported.…”

Section: Introductionmentioning

confidence: 94%

“…In addition, 8HQ derivatives were found to inhibit S. aureus strains 102. Quantitative structure-activity relationships (QSAR) study performed on 24 substituted 8HQ derivatives showed that ten three-dimensional descriptors such as molecular refraction (MR), partition coefficient (logP), total energy (E), standard Gibbs free energy (G), lowest unoccupied molecular orbital (LUMO), highest occupied molecular orbital (HOMO), total molecular energy (TotE), Wien index (WInd), Balaban index (BInd), and octanol-water ClogP were significant for the development of highly predictive ( R 2 = 0.988) model 102. Moreover, potent activity was found in ester derivatives rather than styryl derivatives 102…”

Section: Introductionmentioning

confidence: 99%

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8-Hydroxyquinolines: a review of their metal chelating properties and medicinal applications

Prachayasittikul¹,

Prachayasittikul²,

Ruchirawat³

et al. 2013

DDDT

354

276

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Metal ions play an important role in biological processes and in metal homeostasis. Metal imbalance is the leading cause for many neurodegenerative diseases such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis. 8-Hydroxyquinoline (8HQ) is a small planar molecule with a lipophilic effect and a metal chelating ability. As a result, 8HQ and its derivatives hold medicinal properties such as antineurodegenerative, anticancer, antioxidant, antimicrobial, anti-inflammatory, and antidiabetic activities. Herein, diverse bioactivities of 8HQ and newly synthesized 8HQ-based compounds are discussed together with their mechanisms of actions and structure–activity relationships.

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Section: Introductionmentioning

confidence: 94%

Section: Introductionmentioning

confidence: 99%

8-Hydroxyquinolines: a review of their metal chelating properties and medicinal applications

Prachayasittikul¹,

Prachayasittikul²,

Ruchirawat³

et al. 2013

DDDT

354

276

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show abstract

“… 28 Recently, the anticancer activity of 8HQ-based compounds has been reported. 29 – 33 Moreover, 8HQ and its derivatives exhibit a diverse range of biological activities, such as anti-neurodegenerative, 34 , 35 antimicrobial, 36 – 39 antimalarial, 40 – 42 antioxidant, 30 , 34 anti-inflammatory, 43 and anticancer activities. 44 …”

Section: Introductionmentioning

confidence: 99%

Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinoline and uracil derivatives

Prachayasittikul¹,

Pingaew²,

Nantasenamat³

et al. 2014

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PurposeEstrogens play important roles in the pathogenesis and progression of breast cancer as well as estrogen-related diseases. Aromatase is a key enzyme in the rate-limiting step of estrogen production, in which its inhibition is one strategy for controlling estrogen levels to improve prognosis of estrogen-related cancers and diseases. Herein, a series of metal (Mn, Cu, and Ni) complexes of 8-hydroxyquinoline (8HQ) and uracil derivatives (4–9) were investigated for their aromatase inhibitory and cytotoxic activities.MethodsThe aromatase inhibition assay was performed according to a Gentest™ kit using CYP19 enzyme, wherein ketoconazole and letrozole were used as reference drugs. The cytotoxicity was tested on normal embryonic lung cells (MRC-5) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.ResultsOnly Cu complexes (6 and 9) exhibited aromatase inhibitory effect with IC50 0.30 and 1.7 μM, respectively. Cytotoxicity test against MRC-5 cells showed that Mn and Cu complexes (5 and 6), as well as free ligand 8HQ, exhibited activity with IC50 range 0.74–6.27 μM.ConclusionCu complexes (6 and 9) were found to act as a novel class of aromatase inhibitor. Our findings suggest that these 8HQ–Cu–uracil complexes are promising agents that could be potentially developed as a selective anticancer agent for breast cancer and other estrogen-related diseases.

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Chemoselective synthesis of 5-amino-7-bromoquinolin-8-yl sulfonate derivatives and their antimicrobial evaluation

Krishna¹

2018

Phosphorus, Sulfur, and Silicon and the Related Elements

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Drug Design by Regression Analyses of Newly Synthesized Derivatives of 8-Quinolinol

Abstract: ABSTRACT

Cited by 4 publications

References 11 publications

8-Hydroxyquinolines: a review of their metal chelating properties and medicinal applications

8-Hydroxyquinolines: a review of their metal chelating properties and medicinal applications

Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinoline and uracil derivatives

Chemoselective synthesis of 5-amino-7-bromoquinolin-8-yl sulfonate derivatives and their antimicrobial evaluation

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