Anticancer and anti-inflammatory activities of 1,8-naphthyridine-3-carboxamide derivatives

Srivastava, Sanjay K.; Jaggi, Manu; Singh, Anu; Madan, Alka; Rani, Nidhi; Vishnoi, Manupriya; Agarwal, Shiv Kumar; Mukherjee, Rama; Burman, Anand C.

doi:10.1016/j.bmcl.2007.08.006

Cited by 49 publications

(16 citation statements)

References 6 publications

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“…We selected heterocyclic ring in the main chain and designed ethyl side chain as pendent group of the synthetic polymers to impart certain properties to the polymers. Among different heterocyclic rings, the advantages of using a naphthyridine nucleus and its alkyl side chain include better solubility and biological screening properties 51–54. The new polymers necessitated the synthesis of a new monomer.…”

Section: Resultsmentioning

confidence: 99%

New heteroaromatic polyazomethines containing naphthyridine moieties: Synthesis, characterization, and biological screening

Hussein

Abdelrahman

Geies

2012

J of Applied Polymer Sci

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A new series of heteroaromatic polyazomethines containing 1,8-naphthyridine moieties in the polymer backbone were synthesized with a solution polycondensation technique. A new heteroaromatic monomer containing 1,8-naphthyridine moieties (4-ethoxy-2,7-dicarboxaldehyde-1,8-naphthyridine) was synthesized with an analogous synthetic sequence and confirmed by elemental and spectral data. The resulting polymers were characterized by elemental, spectral analyses, solubility and viscometry measurements. All the synthesized polyazomethines had better solubility in polar aportic solvents. The thermal properties of those polymers were evaluated by thermogravimetric analysis, differential thermogravimetry, and differential thermal analysis measurements and correlated to their structural units. All the polymers had nearly similar maximum polymer decomposition temperatures, which were in the range 557-577 C. A very large differ-ence between the glass transitions (92-222 C) was observed. In addition, with gel permeation chromatography, the molecular weight determination of selected examples of those polymers was evaluated. The values of the average molecular weight for polyazomethines 7 b and 7 c were 34,914 and 24,859, respectively. On the other hand, the biological screening of all of the synthesized polyazomethines was performed in variety of bacteria and fungi. Most of the polyazomethines showed a significant influence against Gram-negative bacteria. The minimum inhibitory concentration of the most active polymers was 0.05 mg/mL.

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Section: Resultsmentioning

confidence: 99%

New heteroaromatic polyazomethines containing naphthyridine moieties: Synthesis, characterization, and biological screening

Hussein

Abdelrahman

Geies

2012

J of Applied Polymer Sci

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“…Our group has specifically explored 1,8-naphthyridine-3-carboxamide derivatives for in vitro anti-inflammatory activity via modulation of the cytokine arm. For the first instance, we demonstrated the inhibitory action of this class of compounds on cytokines TNF-a, MIP-1-a, IL-1-b, IL-6 secreted by key immune cells such as dendritic cells (DC) against LPS-induced levels in vitro [100,101]. Immunostimulatory potential of compounds of this series was also assessed by enhancement of secretion of cytokines in dendritic cellsbased assay from the basal levels [102].…”

Section: Antiviral Activity (Hiv/hcv)mentioning

confidence: 98%

1,8‐Naphthyridine Derivatives: A Review of Multiple Biological Activities

Madaan

Verma

Kumar

et al. 2015

Archiv der Pharmazie

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The 1,8-naphthyridine group of compounds have gained special attention of researchers on account of their demonstrating a variety of interesting biological activities. A wide range of biological properties establishes them as potent scaffolds in therapeutic and medicinal research. The broad spectrum of activities primarily includes antimicrobial, antiviral, anticancer, anti-inflammatory, and analgesic activities. 1,8-Naphthyridine derivatives have also exhibited potential applications in neurological disorders such as Alzheimer's disease, multiple sclerosis, and depression. In addition, these synthetic derivatives have been found to possess activities such as anti-osteoporotic (α(v)β(3) antagonists), anti-allergic, antimalarial, gastric antisecretory, bronchodilator, anticonvulsant, anti-hypertensive, platelet aggregation inhibition, anti-oxidant, EGFR inhibition, protein kinase inhibition, ionotropic agent, β-3 antagonist, MDR modulator, adenosine receptor agonist, adrenoceptor antagonist, and pesticide activities. In spite of the widespread application of the 1,8-naphythyridine scaffolds, only a limited number of review articles are available till date. In this review, we attempt to compile and discuss the key data available in the literature for the multiple biological activities of 1,8-naphthyridine derivatives, in a chronological manner. This review compilation (with 199 references) may be helpful in understanding the diverse biological properties of 1,8-naphthyridines and provide insights into their mechanism of action. This may direct future research in the synthesis of new derivatives and exploring this scaffold for other possible biological activities.

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“…However, further structural exploitations in 1,8-naphthyridine skeleton are required to establish a meaningful structureactivity relationship. Earlier, we have synthesized C-3 carboxamide derivatives with a spacer, which have shown good cytotoxicity along with anti-inflammatory activity [6]. Based on these observations and SAR we have further modified the C-3 carboxamide acid with different amino acid derivatives (4a-d and 8a-c) to afford 1,8-naphthyridine-3-carboxamide derivatives (15-35).…”

Section: Introductionmentioning

confidence: 97%

1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity

Kumar

Jaggi

Singh

et al. 2009

European Journal of Medicinal Chemistry

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Anticancer and anti-inflammatory activities of 1,8-naphthyridine-3-carboxamide derivatives

Cited by 49 publications

References 6 publications

New heteroaromatic polyazomethines containing naphthyridine moieties: Synthesis, characterization, and biological screening

New heteroaromatic polyazomethines containing naphthyridine moieties: Synthesis, characterization, and biological screening

1,8‐Naphthyridine Derivatives: A Review of Multiple Biological Activities

1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity

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