a series of 42 pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinaseinhibitors regarded as promising antitumor agents to complement the existing therapies, wassubjected to a three-dimensional quantitative activity relationship (3d qsar). different qsarmethods, comparative molecular field analysis (comfa), comfa region focusing, andcomparative molecular similarity indices an...

background: renal ischemia reperfusion (ir) injury has been a major source of concern during the past decades and angiotensin converting enzyme (ace) inhibitors have been successfully used to prevent this injury. there have been some controversial reports about the involvement of katp channels in the mechanism of action of ace inhibitors. in this study, we examined the effect of katp channel bl...

background: combination antiplatelet therapy is a classic treatment for percutaneous coronary intervention (pci) but this therapy increases gastrointestinal bleeding (gib). this study highlights the incidence of related risk factors of gib and endoscopic findings in patients with gib after pci and combination antiplatelet therapy. materials and methods: a standard check list was used to evaluat...

background: direct thrombin inhibitors and factor xa inhibitors are gaining popularity as alternatives to warfarin for patients requiring anticoagulation. toxicity due to these medications is difficult to manage because overdose experience is very limited and there is no clear guidance on when or whether to use antidote in this setting. case presentation: a 50-year-old man with normal renal fun...

Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles been very successfully employed to target protein kinases, one of the major druggable families. Here we provide an overview irreversible and reversible covalent kinase clinical development beyond. We further spotlight recent advances t...

Objective: In this paper, we have introduced topoisomerase inhibitors, mechanism of action and types of them. DNA topoisomerases are ubiquitous enzymes that catalyze essential enzymes to solve the topological problems accompanying key nuclear processes such as DNA replication, transcription, repair and chromatin assembly by introducing temporary single or double strand breaks in the DNA. Result...

Objective: In this paper, we have introduced topoisomerase inhibitors, mechanism of action and types of them. DNA topoisomerases are ubiquitous enzymes that catalyze essential enzymes to solve the topological problems accompanying key nuclear processes such as DNA replication, transcription, repair and chromatin assembly by introducing temporary single or double strand breaks in the DNA. Result...

a better understanding of the mechanism of chromosomal aberration formation could be obtained by using dna repair inhibitors. immortalized normal human (mrc 5 svi) and ataxia telangiectasia ( at 5 biv a ) fibroblastic cell lines were treated with adenosine arabinoside (ara-a) and cytosine arabinoside (ara-c), both potent inhibitors of dna dsb repair, alone or in combination with x-rays at g2 or...

bypassing agents are the most commonly used medicines for the treatment of hemophilia patients with inhibitors. the aim of this study is to identify the cost components of management of bleeding vents in hemophilia patients with inhibitors in iran. this study is a cross-sectional study using a bottom-up approach to determine the cost components of treatment of hemophilia patients with inhibitor...