- Evaluation of new chalcone derivatives as polyphenol oxidase inhibitors
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A newly series of 4-(phenylurenyl)chalcone (4a-j) and 4′- (phenylurenyl/thiourenyl)chalcone (9a-l) derivatives were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. Tyrosinase has been purified from banana on an affinity gel comprised of Sepharose 4B-l-tyrosine-p-aminobenzoic acid. The result showed that 4a-j inhibited the PPO enzyme activity. Conversely, 9a-h and 9i-l showed activator effect on tyrosinase enzyme activity.
- Sonmez, Fatih,Sevmezler, Sedat,Atahan, Alparslan,Ceylan, Mustafa,Demir, Dudu,Gencer, Nahit,Arslan, Oktay,Kucukislamoglu, Mustafa
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p. 7479 - 7482
(2012/02/04)
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- Hybrid α-bromoacryloylamido chalcones. Design, synthesis and biological evaluation
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Research into the anti-tumor properties of chalcones has received significant attention over the last few years Two novel large series of α-bromoacryloylamido chalcones 1a-m and 2a-k containing a pair of Michael acceptors in their structures, corresponding to the α-bromoacryloyl moiety and the α,β-unsaturated ketone system of the chalcone framework, were synthesized and evaluated for antiproliferative activity against five cancer cell lines. Such hybrid derivatives demonstrated significantly increased anti-tumor activity compared with the corresponding amino chalcones. The most promising lead molecules were 1k, 1m and 2j, which had the highest activity toward the five cell lines. Flow cytometry with K562 cells showed that the most active compounds resulted in a large proportion of the cells entering in the apoptotic sub-G0-G1 peak. Moreover, compound 1k induced apoptosis through the mitochondrial pathway and activated caspase-3.
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cruz-Lopez, Olga,Cara, Carlota Lopez,Balzarini, Jan,Hamel, Ernest,Canella, Alessandro,Fabbri, Enrica,Gambari, Roberto,Basso, Giuseppe,Viola, Giampietro
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supporting information; experimental part
p. 2022 - 2028
(2009/11/30)
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- PERCHLORIC ACID-ACETIC ACID: A REAGENT SYSTEM FOR DETOSYLATION
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Perchloric acid-acetic acid reagent system has been found to be an efficient reagent for deprotection of p-methyl benzene sulfonyl (tosyl) derivatives of primary aromatic amines, secondary aromatic amines and chiral aminoketones.
- Kudav, D.P.,Samant,S.P.,Hosangadi, B.D.
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p. 1185 - 1188
(2007/10/02)
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