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Synthetic Approaches towards the Sulfonamide Substituted‐1,5‐Diarylimidazole‐2‐thiones as Selective Cyclooxygense‐2 inhibitors
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Latifeh Navidpour Mohsen Amini Ramin Miri Omidreza Firuzi Marjan Tavakkoli Abbas Shafiee 《Journal of heterocyclic chemistry》2014,51(1):71-79
A new series of sulfonamide substituted 1,5‐diarylimidazole, possessing C‐2 alkylthio moiety, were synthesized for their cyclooxygense‐2 (COX‐2) inhibitory activity starting from condensation of N,N‐dibenzylaminosulfonylphenacylamine hydrochloride ( 2 ) and corresponding isothiocyanate in the presence of Et3N, followed by alkylation in the basic medium. In concomitant with these intermediates, 2‐arylamino‐5‐arylthiazole derivatives 5 were also produced. The ratio of these two products was variable with different isothiocyanates. Final debenzylation was achieved using concentrated sulfuric acid to give the title sulfonamides 8 . 相似文献
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Najmeh Edraki Aida Iraji Omidreza Firuzi Yousef Fattahi Mohammad Mahdavi Alireza Foroumadi Mehdi Khoshneviszadeh Abbas Shafiee Ramin Miri 《Journal of the Iranian Chemical Society》2016,13(12):2163-2171
The inhibition of AKR1B10 has been recognized as a potential therapeutic approach to the treatment of various types of cancers. A novel series of compounds with imino-2H-chromen and phenylimino-2H-chromen scaffolds were synthesized by Knoevenagel condensation reaction. The in vitro cytotoxic activity of synthesized compounds was evaluated against MOLT-4 and SK-OV-3 cells. Among the tested compounds, N-(3,4-dimethoxyphenyl)-2-(phenylimino)-2H-chromene-3-carboxamide (8g) demonstrated potent inhibitory activity against both examined cell lines. The results of the molecular docking study suggested that this compound is involved in critical hydrogen-bonding interactions with the Val301 and Lue302 of AKR1B10 catalytic site. 相似文献
3.
Ranjbar Sara Edraki Najmeh Firuzi Omidreza Khoshneviszadeh Mehdi Miri Ramin 《Molecular diversity》2019,23(2):471-508
Molecular Diversity - 5-Oxo-hexahydroquinoline (5-oxo-HHQ) represents a biologically attractive fused heterocyclic core. Various synthetic analogs of 5-oxo-HHQ have been synthesized and assessed... 相似文献
4.
Gatto MT Firuzi O Agostino R Grippa E Borsò A Spinelli F Pavan L Petrolati M Petrucci R Marrosu G Saso L 《Biomedical chromatography : BMC》2002,16(6):404-411
A new assay for the screening of hypochlorite/hypochlorous acid (XOCl) scavengers, based on the reversed-phase high performance liquid chromatographic analysis of human serum albumin (HSA, 0.2% in 100 mM sodium phosphate, pH 7), before and after oxidation by XOCl (1.6 mM), was developed. XOCl induced a significant decrease of the area under the chromatographic peak of HSA at 280 nm due to the oxidation of the aromatic amino acids tryptophan and tyrosine, as suggested by the literature and by the chromatographic analyses and the electrochemical study performed here. The assay was validated by testing known XOCl scavengers such as ascorbic acid, cysteine, glutathione, S-methylglutathione and alpha-lipoic acid and other antioxidants such as carnosine and chlorogenic acid, which inhibited the oxidation of HSA. Quantitative activities were calculated using an original formula based on the changes of the area of the albumin peak. Electrochemical data collected here in a homogeneous medium showed that the anodic potentials of the antioxidants tested are less positive (ascorbic acid, chlorogenic acid and cysteine) or similar (alpha-lipoic acid) compared with those of the aromatic residues (tryptophan and tyrosine) of HSA oxidized by XOCl. However, as expected, carnosine, glutathione and S-methylglutathione were inactive at a glassy-carbon, gold or platinum electrode. 相似文献
5.
Synthesis and Cytotoxic Activity of Some Novel Dihyrobenzo[h]pyrano[3,2‐c]chromene Derivatives
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Nasim Esmati Mahsa Foroughian Mina Saeedi Mohammad Mahdavi Mehdi Khoshneviszadeh Omidreza Firuzi Nader Tanideh Ramin Miri Najmeh Edraki Abbas Shafiee Alireza Foroumadi 《Journal of heterocyclic chemistry》2015,52(1):97-104
Three‐component reaction of 4‐hydroxy‐2H‐benzo[h]chromen‐2‐one, aromatic aldehydes, and malononitrile in the presence of 1,4‐diazabicyclo[2.2.2]octane (DABCO) in ethanol at room temperature affords good yields of novel dihyrobenzo[h]pyrano[3,2‐c]chromene derivatives. The synthesized compounds examined by MTT assays for cytotoxic activity in two human cancer cell lines (MOLT‐4, HL‐60). Most of the evaluated compounds showed low inhibitory activity against tumor cell line at micromolar concentrations. 相似文献
6.
Ranjbar Sara Khoshneviszadeh Mehdi Tavakkoli Marjan Miri Ramin Edraki Najmeh Firuzi Omidreza 《Molecular diversity》2022,26(3):1481-1500
Molecular Diversity - Discovery of novel anticancer agents is of crucial importance to expand the therapeutic options for cancer patients. In this study, a series of 49 5-oxo-hexahydroquinoline and... 相似文献
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Tahmineh Akbarzadeh Saeedeh Noushini Somayeh Taban Mohammad Mahdavi Mahsima Khoshneviszadeh Mina Saeedi Saeed Emami Mohammad Eghtedari Yaghoub Sarrafi Mehdi Khoshneviszadeh Maliheh Safavi Kouros Divsalar Mohammad Hassan Moshafi Ali Asadipour Reyhaneh Sabourian Najmeh Edraki Omidreza Firouzi Ramin Miri Abbas Shafiee Alireza Foroumadi 《Molecular diversity》2015,19(2):273-281
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Quantum dots (QDs) have recently been the focus of attention of many investigators for development of diagnostic tools in many research areas. In this work, we established a new QD-based assay to evaluate the antioxidant/polyphenolic activity. This assay is based on measurement of the inhibitory effect of the antioxidant/polyphenolic compounds on the UV-induced bleaching of CdTe QDs with l-cysteine capping. QDs exhibited excellent photostability without any UV exposure, while they bleached rapidly under UV irradiation. Generation of reactive oxygen species (ROS) under UV irradiation is probably the main cause of the photobleaching of QDs. By comparing the photostability of QDs in buffer solution in the absence and presence of sodium azide, as a known (1)O(2) quencher, the involvement of (1)O(2) in photobleaching of QDs was confirmed. The photobleaching effect induced by ROS could be reduced in the presence of antioxidant/polyphenolic compounds. We tested several antioxidant/polyphenolic compounds as well as known antioxidants such as trolox and 4 different types of tea. The results obtained by the QD-based assay revealed a very good correlation with the data acquired by Folin-Ciocalteu assay. Furthermore, a deeper understanding of the mechanism and the solution for photobleaching of QDs under UV irradiation might be very meaningful in promoting their clinical applications. 相似文献
9.
Rastegari Arezoo Safavi Maliheh Vafadarnejad Fahimeh Najafi Zahra Hariri Roshanak Bukhari Syed Nasir Abbas Iraji Aida Edraki Najmeh Firuzi Omidreza Saeedi Mina Mahdavi Mohammad Akbarzadeh Tahmineh 《Molecular diversity》2022,26(1):409-428
Molecular Diversity - Alzheimer’s disease (AD) is now ranked as the third leading cause of death after heart disease and cancer. There is no definite cure for AD due to the multi-factorial... 相似文献
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