Carbonic anhydrase inhibitors: guaiacol and catechol derivatives effectively inhibit certain human carbonic anhydrase isoenzymes (hCA I, II, IX and XII)
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چکیده
منابع مشابه
Carbonic anhydrase isoenzymes I and II in rabbit erythroid cells.
The morphological and cytochemical changes in erythroid-cell differentiation have been extensively studied: application of the velocity-sedimentation technique has provided preliminary data on the associated biochemical changes (Denton & Arnstein, 1973). After the last cell division there is a dramatic increase in the synthesis of haemoglobin which, at least in part, probably accounts for the a...
متن کاملTargeting carbonic anhydrase IX activity and expression.
Metastatic tumors are often hypoxic exhibiting a decrease in extracellular pH (~6.5) due to a metabolic transition described by the Warburg Effect. This shift in tumor cell metabolism alters the tumor milieu inducing tumor cell proliferation, angiogenesis, cell motility, invasiveness, and often resistance to common anti-cancer treatments; hence hindering treatment of aggressive cancers. As a re...
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Reaction of aromatic/heterocyclic sulfonamides containing a free amino group with triflic anhydride afforded compounds possessing trifluoromethanesulfonamido moieties in their molecule. The Zn(II) and Cu(II) complexes of these new sulfonamides were prepared and characterized by standard procedures (elemental analysis, spectroscopic, magnetic, thermogravimetric and conductimetric measurements). ...
متن کاملMetallocene-based inhibitors of cancer-associated carbonic anhydrase enzymes IX and XII.
In this study, 20 metallocene-based compounds comprising extensive structural diversity were synthesized and evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. These compounds proved moderate to good CA inhibitors in vitro, with several compounds displaying selectivity for cancer-associated isozymes CA IX and CA XII compared to off-target CA I and CA II. Compound 6 was the most potent...
متن کاملTargeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors.
Carbonic anhydrase (CA) enzymes, specifically membrane-bound isozymes CA IX and CA XII, underpin a pH-regulating system that enables hypoxic tumor cell survival and proliferation. CA IX and XII are implicated as potential targets for the development of new hypoxic cancer therapies. To date, only a few small molecules have been characterized in CA-relevant cell and animal model systems. In this ...
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2014
ISSN: 1475-6366,1475-6374
DOI: 10.3109/14756366.2014.956310