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Výsledek výzkumu

Cardioprotective Potential of Iron Chelators and Prochelators

Heart is a particularly sensitive organ to iron overload and cardiomyopathy due to the excessive cardiac iron deposition causes most deaths in disorders such as beta-thalassemia major. Free or loosely bound iron ions readily cycle between ferrous and...

Pharmacology and pharmacy

  • 2019
  • Jimp
  • Odkaz
Výsledek výzkumu

In vitro and in vivo investigation of cardiotoxicity associated with anticancer proteasome inhibitors and their combination with anthracycline

Although proteasome inhibitors (PIs) are modern targeted anticancer drugs, they have been associated with a certain risk of cardiotoxicity and heart failure (HF). Recently, PIs have been combined with anthracyclines (ANTs) to further boost their anti...

Pharmacology and pharmacy

  • 2019
  • Jimp
  • Odkaz
Výsledek výzkumu

Pharmacokinetics of the cardioprotective drug dexrazoxane and its active metabolite ADR-925 with focus on cardiomyocytes and the heart

Dexrazoxane (DEX), the only cardioprotectant approved against anthracycline cardiotoxicity, has been traditionally deemed to be a prodrug of the iron-chelating metabolite ADR-925. However, pharmacokinetic profile of both agents, particularly with res...

Pharmacology and pharmacy

  • 2018
  • Jimp
  • Odkaz
Výsledek výzkumu

Structure-Activity Relationships of Nitro-Substituted Aroylhydrazone Iron Chelators with Antioxidant and Antiproliferative Activities

Aroylhydrazone iron chelators such as salicylaldehyde isonicotinoyl hydrazone (SIH) protect various cells against oxidative injury and display antineoplastic activities. Previous studies have shown that a nitro-substituted hydrazone, namely, NHAPI, d...

Pharmacology and pharmacy

  • 2018
  • Jimp
  • Odkaz
Výsledek výzkumu

2,6-Dihydroxybenzaldehyde analogues of the iron chelator salicylaldehyde isonicotinoyl hydrazone: Increased hydrolytic stability and cytoprotective activity against oxidative stress

Salicylaldehyde isonicotinoyl hydrazone (SIH) is a small molecule and lipophilic chelating agent that firmly binds ferric ions from the cellular labile iron pool and is able to protect various tissues against oxidative damage. Previously, SIH possess...

Pharmacology and pharmacy

  • 2018
  • Jimp
  • Odkaz
Výsledek výzkumu

Investigation of novel dexrazoxane analogue JR-311 shows significant cardioprotective effects through topoisomerase IIbeta but not its iron chelating metabolite

Novel dexrazoxane derivative JR-311 was prepared to investigate structure-activity relationships and mechanism(s) of protection against anthracycline cardiotoxicity. Its cardioprotective, antiproliferative, iron (Fe) chelation and inhibitory and/or d...

Pharmacology and pharmacy

  • 2017
  • Jimp
  • Odkaz
Výsledek výzkumu

Aroylhydrazone iron chelators: Tuning antioxidant and antiproliferative properties by hydrazide modifications

Aroylhydrazones such as salicylaldehyde isonicotinoyl hydrazone (SIH) are tridentate iron chelators that may possess antioxidant and/or antineoplastic activities. Their main drawback, their low stability in plasma, has recently been partially overcom...

FR - Farmakologie a lékárnická chemie

  • 2016
  • Jx
  • Odkaz
Výsledek výzkumu

Characterization of cytoprotective and toxic properties of iron chelator SIH, prochelator BSIH and their degradation products

Free cellular iron catalyzes the formation of toxic hydroxyl radicals and therefore chelation of iron could be a promising therapeutic approach in pathological states associated with oxidative stress. Salicylaldehyde isonicotinoyl hydrazone (SIH) is ...

FR - Farmakologie a lékárnická chemie

  • 2016
  • Jx
  • Odkaz
Výsledek výzkumu

Cardioprotective effects of iron chelator HAPI and ROS-activated boronate prochelator BHAPI against catecholamine-induced oxidative cellular injury

Catecholamines may undergo iron-promoted oxidation resulting in formation of reactive intermediates (aminochromes) capable of redox cycling and reactive oxygen species (ROS) formation. Both of them induce oxidative stress resulting in cellular damage...

FR - Farmakologie a lékárnická chemie

  • 2016
  • Jx
  • Odkaz
Výsledek výzkumu

Large-Scale Synthesis of Piperazine-2,6-dione and Its Use in the Synthesis of Dexrazoxane Analogues

An efficient, large-scale synthesis of piperazine-2,6-dione was developed. The advantages of this procedure include the use of inexpensive starting materials, satisfactory yields, and a convenient workup without the need for chromatographic technique...

CC - Organická chemie

  • 2016
  • Jx
  • Odkaz
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