ChemInform Abstract: Synthesis and Cytotoxicity of New Quinoline Derivatives.

Meshram, H. M.; Reddy, B. Chennakesava; Kumar, Dinesh; Kalyan, Mohit; Ramesh, P.; Kavitha, P.; Rao, J. Venkateswara

doi:10.1002/chin.201304102

Cited by 3 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Quinolines are very important compounds used for new drug development. They are reported as highly selective cytotoxic ( Luo et al, 2009 ; Bawa et al, 2010 ; Meshram et al, 2012 ; Sidoryk et al, 2015 ), broad-spectrum antimicrobial (including activity against Mycobacterium tuberculosis as well as HIV-1 integrase inhibition activity) ( Wang et al, 2019 ), antileishmanial ( Asif, 2014 ), anticonvulsant, anti-inflammatory, cardiovascular activity ( Acharyulu et al, 2008 ; Kumar, Bawa, and Gupta, 2010 ), and have antidiabetic effect ( Shang, et al, 2018a ).…”

Section: Introductionmentioning

confidence: 99%

Eco-Friendly Synthesis, Biological Evaluation, and In Silico Molecular Docking Approach of Some New Quinoline Derivatives as Potential Antioxidant and Antibacterial Agents

et al. 2021

View full text Add to dashboard Cite

A new series of quinoline derivatives 5–12 were efficiently synthesized via one-pot multicomponent reaction (MCR) of resorcinol, aromatic aldehydes, β-ketoesters, and aliphatic/aromatic amines under solvent-free conditions. All products were obtained in excellent yields, pure at low-cost processing, and short time. The structures of all compounds were characterized by means of spectral and elemental analyses. In addition, all the synthesized compounds 5–12 were in vitro screened for their antioxidant and antibacterial activity. Moreover, in silico molecular docking studies of the new quinoline derivatives with the target enzymes, human NAD (P)H dehydrogenase (quinone 1) and DNA gyrase, were achieved to endorse their binding affinities and to understand ligand–enzyme possible intermolecular interactions. Compound 9 displayed promising antioxidant and antibacterial activity, as well as it was found to have the highest negative binding energy of -9.1 and -9.3 kcal/mol for human NAD (P)H dehydrogenase (quinone 1) and DNA gyrase, respectively. Further, it complied with the Lipinski’s rule of five, Veber, and Ghose. Therefore, the quinoline analogue 9 could be promising chemical scaffold for the development of future drug candidates as antioxidant and antibacterial agents.

show abstract

Section: Introductionmentioning

confidence: 99%

Eco-Friendly Synthesis, Biological Evaluation, and In Silico Molecular Docking Approach of Some New Quinoline Derivatives as Potential Antioxidant and Antibacterial Agents

et al. 2021

View full text Add to dashboard Cite

show abstract

“…The nucleophilic aromatic substitution reaction of intermediates 136 with the appropriate amine afforded target compounds 118 – 133 in 42–88% yield (Figure 24) [60].…”

Section: Introductionmentioning

confidence: 99%

The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines

et al. 2019

View full text Add to dashboard Cite

Based on medicinal chemistry tools, new compounds for malaria treatment were designed. The scaffolds of the drugs used to treat malaria, such as chloroquine, primaquine, amodiaquine, mefloquine and sulfadoxine, were used as inspiration. We demonstrated the importance of quinoline and non-quinoline derivatives in vitro with activity against the W2 chloroquine-resistant (CQR) Plasmodium falciparum clone strain and in vivo against Plasmodium berghei-infected mouse model. Among the quinoline derivatives, new hybrids between chloroquine and sulfadoxine were designed, which gave rise to an important prototype that was more active than both chloroquine and sulfadoxine. Hybrids between chloroquine–atorvastatin and primaquine–atorvastatin were also synthesized and shown to be more potent than the parent drugs alone. Additionally, among the quinoline derivatives, new mefloquine derivatives were synthesized. Among the non-quinoline derivatives, we obtained excellent results with the triazolopyrimidine nucleus, which gave us prototype I that inspired the synthesis of new heterocycles. The pyrazolopyrimidine derivatives stood out as non-quinoline derivatives that are potent inhibitors of the P. falciparum dihydroorotate dehydrogenase (PfDHODH) enzyme. We also examined the pyrazolopyridine and pyrazolopyrimidine nuclei.

show abstract

“…In another study, Meshram et al showed that some quinoline derivatives they had prepared were toxic to human cell line HL-60 (myeloid leukemia) and U937 (leukemic monocyte lymphoma) (20). To the best of our knowledge, in all articles we reviewed in literature, the authors have reported the syntheses of quinoline derivatives and investigated their cytotoxic properties against different human cancer cell lines.…”

Section: Introductionmentioning

confidence: 99%

Can Functionalization of Quinoline Derivatives Be Exploited to Control Quinolines Cytotoxic Effects?

Hami

Zibaseresht

2017

J Arch Mil Med

View full text Add to dashboard Cite

Background: Quinoline and its variety of derivatives have long been studied for their biological activities such as anticancer, antitumor, anti-inflammatory, and antioxidant properties. Objectives: As part of our research, we are interested in the synthesis and development of heterocyclic compounds such as quinoline derivatives and poly-pyridyl materials that might have potential biological activities. Particularly, anti-cancerous and antibacterial properties of such compounds are of our interest. Methods: A previously synthesized mixture of two quinoline derivative isomers (7-methylquinoline and 5-methylquinoline (A + B)) and other four quinoline derivatives (7-methyl-8-nitro-quinoline (C), 7-(β-trans-(N,N-dimethylamino) ethenyl) -8-nitroquinoline (D), 8-nitro-7-quinolinecarbaldehyde (E), and 8-Amino-7-quinolinecarbaldehyde (F)) were selected to evaluate their in vitro cytotoxicity against human epithelial colorectal carcinoma (Caco-2) cultured cells by MTT assay. The IC50 values for the mixture and other compounds were calculated by SigmaPlot 12.0 software.

show abstract

ChemInform Abstract: Synthesis and Cytotoxicity of New Quinoline Derivatives.

Cited by 3 publications

References 0 publications

Eco-Friendly Synthesis, Biological Evaluation, and In Silico Molecular Docking Approach of Some New Quinoline Derivatives as Potential Antioxidant and Antibacterial Agents

Eco-Friendly Synthesis, Biological Evaluation, and In Silico Molecular Docking Approach of Some New Quinoline Derivatives as Potential Antioxidant and Antibacterial Agents

The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines

Can Functionalization of Quinoline Derivatives Be Exploited to Control Quinolines Cytotoxic Effects?

Contact Info

Product

Resources

About