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| 1 | Chalcone analogue as potent anti-malarial compounds against Plasmodium falciparum:Synthesis,biological evaluation,and docking simulation study显示文摘Objective: To investigate in vitro antimalarial activity of chalcone derivative compounds against Plasmodum falciparum 3D7(Pf3D7) strain and in silico antimalarial activity.Methods: Synthesis of the chalcone derivatives was conducted via Claisen-Schmidt method using NaOH 60% base as catalyst. An in vitro antimalarial activity assay was carried out according to the Rieckmann method against the chloroquine-sensitive Pf3D7 strain. Molecular docking studies of the prepared compounds were performed using Discovery Studio 3.1(Accelrys, Inc., San Diego, USA) software to dihydrofolate reductases-thymidylate synthase(PfDHFR-TS) protein with Protein Data Bank ID of 1J3I.pdb(sensitive-protein) and ID: 4DP3.pdb(resistance-protein).Results: This work has successfully synthesized seven chalcone derivatives with a great antimalarial activity. It has been revealed that allyloxy, hydroxy and alkoxy functional groups could increase the antimalarial activity of the chalcone derivatives. The best antimalarial activity of the prepared compounds was possessed by 3b with an IC_(50) value of 0.59 μM and categorized as an excellent antiplasmodial. Molecular docking studies of 3b showed binding interaction with the amino acid residues such as Ala16. Ile 164. Phe58.Tyr170 of the 1J3I.pdb protein and also Ala16, Phe58, Ile 112, Met55 of the 4DP3.pdb protein.Conclusions: An in vitro antimalarial assay of the prepared chalcone derivative(3a-g)showed an excellent and good antiplasmodial activity against the chloroquine-sensitive Pf3D7 strain. In silico antimalarial studies revealed that 3a-g made binding interaction with both sensitive-protein(IJ3I.pdb) and resistance-protein(4DP3.pdb), which means that they were both active against chloroquine-sensitive and resistant plasmodium strain. | Jufrizal Syahri Emmy Yuanita Beta Achromi Nurohmah Ria Armunanto Bambang Purwono | 2017 | Asian Pacific Journal of Tropical Biomedicine2017，7，8： | 3 |
| 2 | Measurement of anthocyanins and other phytochemicals in purple wheat 显示文摘 | Hosseinian F S Li W Beta T | 2008 | Food Chemistry2008，109，4： | 1 |
| 3 | Maternal serum placental protein 13 at 11-13 weeks of gestation in preeclampsia显示文摘 | Akolekar R Syngelaki A Beta J et a/ | 2009 | Prenat Diagn2009，29，12： | 1 |
| 4 | Microstructure of Fe-Cr-C hardfacing alloy with additions of Nb, Ti, B 显示文摘 | Betas H Fischer A | 1997 | Materials Characterization1997，39，24： | 1 |
| 5 | Radiocontrast media associated nephrotoxicity显示文摘 | Betas J Rudnick M | 1992 | Kidney1992，24，： | 1 |
| 6 | Th17 cytokines are critical for respiratory syneytial virus-associated airway hyperreponsiveness through regulation by complement C3a and tachykinins显示文摘 | Beta MM Lu B Martin TR | 2011 | J Im- munol2011，187，8： | 1 |
| 7 | A trial of the beta-blocker bucindolol in patients with advanced chronic heart failuer显示文摘 | The beta bilcker Evaluation of Survival Trial Investigators | 2001 | N End J Med2001，344，22： | 1 |
| 8 | Protein characteristics of Chinese black-grained wheat显示文摘 | Wende Li Trust Beta Shancheng Sun Harold Corke | 2005 | Food Chemistry2005，，3： | 1 |
| 9 | HFA protein and SMRP: Potential novel biomarkers in ovarian cancer detection 显示文摘 | Fritz-Rdzanek A Grzybowski W Beta J | 2012 | Oncol Lett2012，4，3： | 1 |
| 10 | Genomic profiling by array comparative genomic hybridization reveals novel DNA copy number changes in breast phyllodes tumours 显示文摘 | Kuijper A Snijders AM Betas EM | 2009 | Cell Oncol2009，31，1： | 1 |
| 11 | Starch properties as affvctcd by sorghum grain chemistry显示文摘 | BETA T CORKE H ROONEY L W | 2001 | Journal of the Science of Food and Agriculture2001，81，： | 1 |
| 12 | Effect of steeping treatment on pasting and thermal properties of sorghum starches显示文摘 | TRUST BETA HAROLD CORKE JOHN R N TAYLOR | 2001 | Cereal Chem2001，78，3： | 1 |
| 13 | A genetic screen identifies pitxl as a suppressor of ras activity and tumorigenicity显示文摘 | Koffschoten IG van Leeuwen B Betas K | 2005 | Cell2005，121，6： | 1 |
| 14 | Watershed-scale hydrologic and non- point-source pollution models: Review of applications显示文摘 | Borah D K Beta M | 2004 | Transactions of the ASAE2004，47，3： | 1 |
| 15 | Effects of pre-dehullingtreatments on some nutritional and physical properties of navyand pinto beans (Phaselous vulgaris ) 显示文摘 | Anton A A Ross K A Beta T | 2008 | Food Science andTechnologyf2008，41，5： | 1 |
| 16 | Simple Diagnostic Tests for Spatial Depen- dence显示文摘 | Anselin L Beta A K R | 1996 | Regional Science and Urban Economics1996，，1： | 1 |
| 17 | Selection and dosing of medications for management of diabetes in patients with advanced kidney disease 显示文摘 | Reilly JB Betas JS | 2010 | Semin Dial2010，23，2： | 1 |
| 18 | Laser scissors and tweezers 显示文摘 | Betas M W Tadir Y Liang H | 1998 | Methods in cell biology1998，55，： | 1 |
| 19 | Dysfunctional uterine bleeding- diagnostics and treatment 显示文摘 | Jakimiuk A J Grzybowski W Beta J | 2008 | Ginekol Pol2008，79，4： | 1 |
| 20 | Photodynamic effects on human and chicken erythrocytes studied with microirradiation and confocal laser scanning microscopy 显示文摘 | Konig K Kimel S Betas MW | 1996 | Laser Surg Med1996，19，： | 1 |
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