Synthesis, in vitro antimalarial activity and cytotoxicity of novel 4-aminoquinolinyl-chalcone amides

Smit, Frans J.; N’Da, David D.

doi:10.1016/j.bmc.2013.12.032

Cited by 54 publications

(21 citation statements)

References 38 publications

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“…Eight of the total synthesized compounds were observed to be potent with IC 50 Chalcone amides containing quinoline ring 72 were synthesized and in vitro screening was performed against the CQ-resistant (W2) and CQ-sensitive (3D7) strains of P. falciparum [81] along with their cytotoxicity evaluation against the normal human foetal lung fibroblast cell line (WI-38) (Fig. 19).…”

Section: Anti-malarial Activitymentioning

confidence: 99%

Recent developments in biological activities of chalcones: A mini review

Singh

Ȧnand

Kumar

2014

European Journal of Medicinal Chemistry

601

319

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Section: Anti-malarial Activitymentioning

confidence: 99%

Recent developments in biological activities of chalcones: A mini review

Singh

Ȧnand

Kumar

2014

European Journal of Medicinal Chemistry

601

319

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“…The furan‐containing chalcone–quinoline hybrids 37 (IC 50 : 50–460 nM) demonstrated great potency against CQS 3D7 and CQR W2 P. falciparum strains. [ 81 ] The SAR indicated that extension of the alkyl linker could boost up the activity, but replacement of alkyl linker by the ether and alkylamino linkers had little impact on the activity. Hybrid 37d (IC 50 : 50 and 70 nM) was found to be most active against CQS 3D7 and CQR W2 strains, and the activity was not inferior to that of chloroquine (IC 50 : 50 and 120 nM).…”

Section: Chalcone–quinoline Hybridsmentioning

confidence: 99%

Chalcone hybrids and their antimalarial activity

Cheng

Yang

Huang

et al. 2020

Archiv der Pharmazie

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Malaria, one of the most striking, re‐emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug‐resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure–activity relationship of these compounds are also discussed.

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“…The antiplasmodial SAR of quinoline‐chalcone hybrids 64 (IC 50 : 50‐1780 nM) indicated that the activity against CQS D10 and CQR D2 strains was closely associated with length of diaminoalkyl linker, and extension of the length was favorable to the activity . Among them, the most active hybrid 64e (IC 50 : 50 and 70 nM) was as potent as CQ (IC 50 : 50 nM) against CQS D10 strain, and 1.7‐fold more potent than CQ (IC 50 : 120 nM) against CQR D2 strain.…”

Section: Quinoline Hybridized With Novel Antimalarial Pharmacophores mentioning

confidence: 99%

Hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug‐resistant Plasmodium falciparum

Feng

Chang

et al. 2019

Medicinal Research Reviews

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Malaria is a tropical disease, leading to around half a million deaths annually. Antimalarials such as quinolines are crucial to fight against malaria, but malaria control is extremely challenged by the limited pipeline of effective pharmaceuticals against drug-resistant strains of Plasmodium falciparum which are resistant toward almost all currently accessible antimalarials. To tackle the growing resistance, new antimalarial drugs are needed urgently. Hybrid molecules which contain two or more pharmacophores have the potential to overcome the drug resistance, and hybridization of quinoline privileged antimalarial building block with other antimalarial pharmacophores may provide novel molecules with enhanced in vitro and in vivo activity against drug-resistant (including multidrug-resistant) P falciparum. In recent years, numerous of quinoline hybrids were developed, and their activities against a panel of drug-resistant P falciparum strains were screened. Some of quinoline hybrids were found to possess promising in vitro and in vivo potency. This review emphasized quinoline hybrid molecules with

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Synthesis, in vitro antimalarial activity and cytotoxicity of novel 4-aminoquinolinyl-chalcone amides

Cited by 54 publications

References 38 publications

Recent developments in biological activities of chalcones: A mini review

Recent developments in biological activities of chalcones: A mini review

Chalcone hybrids and their antimalarial activity

Hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug‐resistant Plasmodium falciparum

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