- Glyoxalase 1 and 2 enzyme inhibitory activity of 6-sulfamoylsaccharin and sulfocoumarin derivates
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The glyoxalase enzymes represent a cellular defence system against the accumulation of cytotoxic α-oxoaldehydes leading to apoptosis. The potential of glyoxalase inhibitors to act as novel anti-cancer agents for drugresistant tumours that over-express gly
- Makrecka, Marina,Zalubovskis, Raivis,Vavers, Edijs,Ivanova, Jekaterina,Grandane, Aiga,Dambrova, Maija
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p. 410 - 414
(2013/07/26)
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- Synthesis of 6-sulfamoylsaccharin and study of its reactivity in alkylation reactions
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An improved method for the preparation of 6-sulfamoylsaccharin (3-oxo-2,3-dihydro-1,2-benzothiazole-6-sulfonamide 1,1-dioxide) has been developed and studies of its possible direct alkylation have been carried out. It was shown that alkylation occursregio
- Ivanova,Simin, E. Yu.,Vozny,Trapencieris,?alubovskis
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p. 1561 - 1564
(2018/01/27)
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- Design, synthesis and biological evaluation of benzo[1.3.2]dithiazolium ylide 1,1-dioxide derivatives as potential dual cyclooxygenase-2/5-lipoxygenase inhibitors
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3-(4-Bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide (5) was discovered as a new prototype for dual inhibitors of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). Thus, the structure-activity relationships of benzo[1.3.2]dithiazolium ylide 1,1-dioxide skeleton were carried out. The 6-NO2 group played an essential role in the inhibitory activity. In addition, moderate-sized lipophilic substituents at the para-position of the 3-aryl moiety were required for dual COX-2/5-LOX inhibitory activity. Among the identified potent dual inhibitors, 3-(4-tbutylphenyl) derivative 30c (IC50 values of 0.27 μM and 0.30 μM against COX-2 and 5-LOX, respectively) and 3-(4-biphenyl) derivative 30f (IC50 values of 0.50 μMand 0.15 μMagainst COX-2 and 5-LOX, respectively) were the most potent dual COX-2/ 5-LOX inhibitors. Intraperitoneal administration of 30c at 100 mg/kg demonstrated potent acute antiinflammatory activity. As a result, benzo[1.3.2]dithiazolium ylide 1,1-dioxide represented a novel scaffold for the exploitation in developing dual COX-2/5-LOX inhibitors.
- Tan, Chen-Ming,Chen, Grace Shiahuy,Chen, Chien-Shu,Chang, Pei-Teh,Chern, Ji-Wang
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experimental part
p. 6316 - 6328
(2011/12/02)
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