The diarylurea is a scaffold of great importance in medicinal chemistry as it present numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine inhibitors, were recently reported literature. first to come into the market an anticancer agent was sorafenib, followed by some others. In t...

Second generation tyrosine kinase inhibitors have recently been introduced as first-line treatment for chronic phase chronic myelogenous leukemia. We aimed to evaluate the efficacy and safety of 2(nd) generation tyrosine kinase inhibitors versus imatinib as first-line treatment for these patients. We carried out a systematic review and meta-analysis of randomized controlled trials comparing 2(n...

background: the secondary genetic changes other than the promyelocytic leukemia-retinoic acid receptor (pml-rara) fusion gene may contribute to the acute promyelocytic leukemogenesis. chromosomal alterations and mutation of flt3 (fms-like tyrosine kinase 3) tyrosine kinase receptor are the frequent genetic alterations in acute myeloid leukemia. however, the prognostic significance of flt3 mutat...

The management of patients with chronic myeloid leukemia (CML) during pregnancy has become recently a matter of continuous debate. The introduction of the Tyrosine Kinase Inhibitors (TKIs) in clinical practice has dramatically changed the prognosis of CML patients; in fact, patients diagnosed in chronic phase can reasonably expect many years of excellent disease control and good quality of life...

The ErbB RTKs (EGFR, HER2, HER3, and HER4) have been well-studied in cancer. EGFR, HER3 stimulate cancer proliferation, principally by activating the phosphatidylinositol-3-kinase extracellular signal-regulated kinase (ERK) pathways, resulting increased cell survival proliferation. Cancer cells high densities of causing phosphorylation tyrosine amino acids on protein substrates near C-terminal ...

Steady-state enzyme kinetics is a cornerstone technique of biochemistry and related sciences since it allows the characterization quantification behaviour. Enzyme widely used to investigate physiological role enzymes, determine effects mutations characterize inhibitors. Well-known examples inhibitors treat diseases include anti-infectives (e.g., penicillin, clavulanic acid HIV protease inhibito...

The purpose of this study was to determine whether inhibitors of tyrosine kinase attenuate vasodilation elicited by endogenously elaborated and exogenously applied nitric oxide in the in situ peripheral microcirculation. Using intravital microscopy, we found that pretreatment with genistein (1.0 microM) and tyrphostin 25 (10.0 microM), two structurally unrelated tyrosine kinase inhibitors, sign...

Pancreatic cancer has proven to be chemo-resistant, with gemcitabine being the only cytotoxic agent approved for advanced pancreatic cancer since 1996. Tyrosine kinase inhibitors represent a newer generation of chemotherapeutic agents targeting specific tumor pathways associated with carcinogenesis including cell cycle control, signal transduction, apoptosis and angiogenesis. These agents prese...

The use of interferon-a (INF) in chronic myeloid leukemia, when it started in the 80s, was considered as a breakthrough in the therapy of this disease; INF administered alone or in combination with aracytin was the standard choice for treatment for Chronic Myeloid Leukemia (CML) patients unfit for bone marrow transplantation. With the appearance of the first Tyrosine Kinase Inhibitor (TKI) (ima...