Efficient Synthesis and Evaluation of Antitumor Activities of Novel Functionalized 1,8-Naphthyridine Derivatives

Fu, Lei; Feng, Xiujuan; Wang, Jianjun; Zhan, Xun; Hu, Jundie; Zhang, Juanjuan; Zhao, Yiming; Huang, Zhibin; Shi, Daqing

doi:10.1021/co500120b

Cited by 53 publications

(17 citation statements)

References 56 publications

(19 reference statements)

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“…Duggan et al [78] synthesize and study SAR of the CB1 receptor adverse agonists derived from dihydro-pyrano [2, 3-b] pyridine and tetrahydro-1, 8-naphthyridine scaffolds. Rat food intake and pharmacokinetic study of compound (63) shows that tetrahydro-1, 8-naphthyridine bicyclic core structures, are orally useful in regulation of food intake and body weight in a rodent model.…”

Section: Cb1 Receptor Inverse Agonistsmentioning

confidence: 99%

Recent Developments and Multiple Biological Activities Available With 1, 8-Naphthyridine Derivatives: A Review

Gurjar¹,

Pal²

2019

Int J Pharm Pharm Sci

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Within the wide range of nitrogen-containing heterocyclic compounds, the derivatives of 1,8-naphthyridine (NPTR) have gained a rising interest due to their reported versatile biological activities. The derivatives of NPTR scaffold are found to invite special interest from researchers nowadays on the significance of their manifestations of multiple attractive pharmacological activities which establish them as an effective and versatile tool in pharmaceutical chemistry and drug discovery. The diverse biological activities mainly include anti-inflammatory, antimicrobial, antiviral, anticancer, antihypertensive and analgesic activities. Novel NPTR scaffold has emerged its potency to treat neurological diseases like depression and Alzheimer's disease. Further these agents possess different inhibitory activities, such as anti-HIV, anti-osteoporotic, αvβ3 antagonism, antimalarial, platelet aggregation, anti-oxidant, anti-allergic, gastric antisecretory, anticonvulsant, epidermal growth factor receptor (EGFR) inhibition, protein kinase inhibition, ionotropic properties, β3 antagonism, phosphodiesterase 4 (PDE 4) inhibitions, adenosine receptor agonistic activity, adrenoceptors antagonism and DNA stabilizing activity, etc. In this review, we highlight the updates of different 1,8-naphthyridine derivatives and explain the key data available in the context of various biological activities of NPTR derivatives available from the literature. This may direct opportunity in researches in the synthesis of novel medicinal agents and the development of new heterocycles for modification of existing biological actions as well as evaluation of other possible pharmacological activities.

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Section: Cb1 Receptor Inverse Agonistsmentioning

confidence: 99%

Recent Developments and Multiple Biological Activities Available With 1, 8-Naphthyridine Derivatives: A Review

Gurjar¹,

Pal²

2019

Int J Pharm Pharm Sci

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“…All of the newly synthesized compounds were evaluated for their in vitro antiproliferative properties against cancer; several compounds were found to have high activities (Scheme 36). 59 A synthetic route of novel highly substituted cyclopentadienes containing quinoline nucleus was described, in which a Knoevenagel adducts 104a-c of 2-chloroquinoline-3-carbaldehydes I and malononitrile or ethyl cyanoacetate were prepared. The reaction mixture was stirred in ethanol for 15 min at room temperature.…”

Section: Scheme 34mentioning

confidence: 99%

2-Chloroquinoline-3-carbaldehydes: synthesis and reactions (2012-2017)

Massoud¹,

Bayoumi²,

Farahat³

et al. 2018

Arkivoc

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“…The relation between surviving cells and drug concentration is plotted to get the survival curve of each tumor cell line after treatment with the specified compound. The 50% inhibitory concentration (IC 50 ), the concentration required to cause toxic effects in 50% of intact cells, was estimated from graphic plots of the dose response curve for each concentration using Graphpad Prism software (San Diego, CA, USA) [47,48].…”

Section: Antitumor Activity Assaymentioning

confidence: 99%