Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials

Joshi, Advait A.; Narkhede, Sachin S.; Viswanathan, C. L.

doi:10.1016/j.bmcl.2004.10.037

Cited by 76 publications

(38 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Novel 5-substituted amino-2,4-diamino-8-chloropyrimido- [4,5-b]quinolines 172 were designed based upon a pharmacophore developed using Chem-X and MOE softwares. The designed molecules were synthesized and evaluated by Rane's test for blood-schizontocidal activity in mice infected by P. berghei.…”

Section: F New Structural Classes Of Antimalarial Agentsmentioning

confidence: 99%

Recent advances in antimalarial drug development

Vangapandu

Jain

Kaur

et al. 2006

Medicinal Research Reviews

View full text Add to dashboard Cite

Malaria caused by protozoa of the genus Plasmodium, because of its prevalence, virulence, and drug resistance, is the most serious and widespread parasitic disease encountered by mankind. The inadequate armory of drugs in widespread use for the treatment of malaria, development of strains resistant to commonly used drugs such as chloroquine, and the lack of affordable new drugs are the limiting factors in the fight against malaria. These factors underscore the continuing need of research for new classes of antimalarial agents, and a re-examination of the existing antimalarial drugs that may be effective against resistant strains. This review provides an in-depth look at the most significant progress made during the past 10 years in antimalarial drug development.

show abstract

Section: F New Structural Classes Of Antimalarial Agentsmentioning

confidence: 99%

Recent advances in antimalarial drug development

Vangapandu

Jain

Kaur

et al. 2006

Medicinal Research Reviews

View full text Add to dashboard Cite

show abstract

“…Many heterocyclic units contain quinoline scaffold as an integral part and show antiviral [7], antimalarial [8][9][10], antibacterial [8][9][10][11][12][13] and anticancer activities [14]. Conventional methods for the synthesis of quinoline and its derivatives reported in the literature include Skraup [15], Doebner-Von Miller [16], Friedlander [17] and Combes synthesis.…”

Section: Introductionmentioning

confidence: 99%

Quantitative Structure Activity Relationship and Biological Activity Studies of 4-Methyl-2-(4-substituted phenyl)quinoline Derivatives

Rahangdale¹,

Inam²,

Chourasia³

2018

Asian J. Chem.

View full text Add to dashboard Cite

Quantitative structure activity relationship (QSAR) studies of some 4-methyl-2-(4-substituted phenyl)quinoline derivatives were carried out to determine their predicted biological activities. Numbers of descriptors were tested to adjudge a quantitative correlation between activity and structural features using training set and test set. Significant correlation was observed between activities and descriptors. The results were interpreted on the basis of linear regression analysis. Experimental antibacterial activities of the test set compounds were determined. The predicted biological activities generated by QSAR model were compared with the experimental antibacterial activities. The concurrence between the predicted and experimental biological activities validates the QSAR model. Thus, it can be concluded that the model under the present investigation can be applied for predicting the unknown biological activities of structurally similar molecules.

show abstract

“…Quinoline derivatives posses a wide range of biological activities including anti-inflammatory [1], antileishmanial [2], antifungal [3], antituberculosis [4], and antimalarial activities [5,6]. Also, several novel quinoline derivatives have been reported to show substantial anticancer activities [7][8][9][10][11][12][13][14].…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of some novel quinoline derivatives as anticancer and radiosensitizing agents targeting VEGFR tyrosine kinase

Ghorab

Ragab

Heiba

et al. 2011

Journal of Heterocyclic Chem

View full text Add to dashboard Cite

in Wiley Online Library (wileyonlinelibrary.com).Quinoline derivatives posses many types of biological activities and have been reported to show significant anticancer activity. There is a variety of mechanisms for the anticancer activity and the most distinguished mechanism is the inhibition of vascular epithelial growth factor receptor tyrosine kinase (VEGFRTK). Novel quinoline derivatives 6-12 and pyrimido [4,5-b]quinoline derivatives 16-20 are reported herein. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7) in which VEGFR is highly expressed. Compounds 6 and 7 with IC 50 values of 8.5 lM and 21.9 lM were the most active compounds and exhibited cytotoxic activities higher than that of the reference drug doxorubicin (IC 50 ¼ 32.02 lM). The most active compounds 6 and 7 were further evaluated for their ability to enhance the cell killing effect of c-radiation.

show abstract

Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials

Cited by 76 publications

References 3 publications

Recent advances in antimalarial drug development

Recent advances in antimalarial drug development

Quantitative Structure Activity Relationship and Biological Activity Studies of 4-Methyl-2-(4-substituted phenyl)quinoline Derivatives

Design and synthesis of some novel quinoline derivatives as anticancer and radiosensitizing agents targeting VEGFR tyrosine kinase

Contact Info

Product

Resources

About