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RISS 인기검색어
- 검색키워드
- 저자 : Najmeh Edraki (검색결과 3 건)
- 무료
- 기관 내 무료
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Cytotoxic Activity Evaluation and QSAR Study of Chromene-based Chalcones
Loghman Firoozpour,Alireza Foroumadi,Najmeh Edraki,Maryam Nakhjiri,Saeed Emami,Maliheh Safavi,Sussan Kabudanian Ardestani,Mehdi Khoshneviszadeh,Abbas Shafiee 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.12
Chalcone and chromene motifs are synthetic or naturally occurring scaffolds with significant cytotoxic profile. Two types of novel regioisomeric chromene-chalcone hybrids, namely 1-(6-chloro or 6-methoxy-2H-chromen-3-yl)-3-phenylprop-2-en-1-one (Type A) and 3-(6-chloro or 6-methoxy-2H-chromen-3-yl)-1-phenylprop-2-en-1-one (Type B), both with different substituents on the phenyl ring attached to propenone linkage, have been evaluated for their cytotoxic activity against breast cancer cell lines (MCF-7 and MDA-MB-231). The results indicate that type A of chromene-chalcones demonstrated better cytotoxic profile than type B especially in MDA-MB-231 cell line. In addition, the growth inhibitory activity of most of the target compounds is higher than Etoposide as a reference drug. QSAR analysis of these novel compounds demonstrated that topological and geometrical parameters are among the important descriptors that influence the cytotoxic activity profile of compounds.
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Ramin Miri,Omidreza Firuzi,Nima Razzaghi-Asl,Katayoun Javidnia,Najmeh Edraki 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.4
b-site amyloid precursor protein cleavingenzyme (BACE-1) is a validated target for Alzheimer therapydue to its distinctive role in pathogenesis of AD. In thepresent contribution, a series of new 3,5-bis-N-(aryl/heteroaryl)carbamoyl-4-aryl-1,4-dihydropyridine structureswere synthesized as BACE-1 inhibitors (6a–6n). In vitroBACE-1 inhibitory activities were determined by enzymaticfluorescence resonance energy transfer assay. Synthesizeddihydropyridine (DHP) analogues exhibited weak to goodinhibitory activities while 6i, 6n and 6a were found to be themost potent molecules with 83.76, 79.45 and 72.47 %BACE-1 inhibition at 10 lM, respectively. Structure binding/activity relationship elucidations revealed that superiorBACE-1 inhibitory activities were observed for DHPderivatives bearing fused/non-fused thiazole groups andparticularly 3,5-bis-N-(6-ethoxy-2-benzothiazolyl) moiety. Binding maps showed that enhanced activity may beattributed to the additional H-bond and hydrophobic interactionswith S2–S3 subpockets of BACE-1.
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Hasti Sarkarzadeh,Ramin Miri,Omidreza Firuzi,Mohsen Amini,Nima Razzaghi-Asl,Najmeh Edraki,Abbas Shafiee 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.4
A series of new imidazole substituted indeno[1,2-b]quinoline-9,11-dione derivatives were synthesizedand evaluated for their antiproliferative effects on HeLa,LS180, MCF-7 and Jurkat human cancer cell lines. Antiproliferativeeffects were evaluated using MTT assay. Prepared compounds exhibited weak to good antiproliferativeactivity in evaluated cell lines. Prepared compoundswere more potent in Jurkat cell line when compared toLS180, HeLa and MCF-7 cell lines. Compounds 29(IC16 = 0.7 lM) and 31 (IC16 = 1.7 lM) and 33 (IC16 =1.7 lM) were found to be the most potent molecules onJurkat cell lines. Moreover; it was found that some of thetested compounds bearing imidazole-2-yl moiety on theC11-position of dihydropyridine ring exhibited superiorantiproliferative activity in comparison to cis-platin especiallyin Jurkat cell line (compounds 29, 31, and 33). Itseemed that the introduction of electron-withdrawinggroups on the imidazole ring enhanced the antiproliferativepotential of these compounds (compounds 27, 29 and 31). The results of this study proposed that some of the imidazolesubstituted indeno[1,2-b]quinoline-9,11-dione compoundsmay act as efficient anticancer agents in vitro,emphasizing their potential role as a source for rationaldesign of potent antiproliferative agents.
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