1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents.

A class of substituted 1-thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives was found to have potent anti-proliferative activity against a broad range of tumor cell lines. A compound from this class (14) was profiled across a broad panel of hematologic and solid tumor cancer cell lines demonstrating cell cycle arrest at the G0/G1 interphase and has potent anti-proliferative activity against a distinct and select set of cancer cell types with no observed effects on normal human cells. An example is the selective inhibition of human B-cell lymphoma cell line (BJAB).

Immune response to sipuleucel-T in prostate cancer.

Historically, chemotherapy has remained the most commonly utilized therapy in patients with metastatic cancers. In prostate cancer, chemotherapy has been reserved for patients whose metastatic disease becomes resistant to first line castration or androgen deprivation. While chemotherapy palliates, decreases serum prostate specific antigen and improves survival, it is associated with significant side effects and is only suitable for approximately 60% of patients with castrate-resistant prostate cancer.

Preoperative haemodynamic parameters and the immediate outcome after open repair of ruptured abdominal aortic aneurysms.

Aim: The aim of this study was to evaluate the impact of preoperative cardiac function and haemodynamic parameters on the immediate outcome after repair of ruptured abdominal aortic aneurysm (RAAA).

Methods: This is a retrospective review of 68 consecutive patients who underwent emergency repair of RAAA. Baseline pulmonary artery pressure, cardiac index, oxygen saturation and pulse rate were measured and recorded immediately after insertion of a pulmonary artery thermodilution catheter and before anaesthesia induction.

Repeat intervention after invasive treatment of coronary arteries.

Objective: Patients who undergo successful revascularisation either with coronary artery bypass grafting (CABG) or with percutaneous coronary intervention (PCI) may subsequently require repeat invasive procedures.

Methods: A cohort of 662 coronary artery diseased (CAD) patients was retrospectively reviewed. Follow-up was 36 months.

HRQoL after coronary artery bypass grafting and percutaneous coronary intervention for stable angina.

Objectives: To assess the health related quality of life (HRQoL) and the change in the NYHA class after coronary artery bypass grafting (CABG) or percutaneous coronary intervention (PCI) in the management of stable coronary artery disease (CAD). The study was non-randomized. CABG group consisted of 240 patients and 229 patients were treated with PCI.

Postoperative delirium and health related quality of life after coronary artery bypass grafting.

Objectives: We wanted to identify determinants for postoperative delirium and its influence on health related quality of life (HRQoL) during 36-month follow-up of coronary artery bypass (CABG) patients.

Design: A total of 302 patients were retrospectively analyzed. HRQoL was assessed prospectively by the 15D instrument.

EuroSCORE predicts health-related quality of life after coronary artery bypass grafting.

Three hundred and two patients were evaluated for the EuroSCORE risk and health-related quality of life (HRQoL) during three years after CABG as assessed by the 15D instrument. Both additive and logistic EuroSCORE correlated significantly with the 15D score at 6, 18 and 36 months. A clinically important increase > or =0.

Quality of life during 18 months after coronary artery bypass grafting.

Objective: The aim of the present study was to evaluate the change in health related quality of life (HRQoL) among elective coronary artery bypass grafting (CABG) patients.

Methods: A total of 302 CABG patients were included in the study. Complete pre-, peri- and postoperative data were collected comprehensively in a database.

Risk-scoring method for prediction of 30-day postoperative outcome after infrainguinal surgical revascularization for critical lower-limb ischemia: a Finnvasc registry study.

Background: The aim of the present study was to develop a risk-scoring method for prediction of immediate postoperative outcome after infrainguinal surgical revascularization for critical limb ischemia.

Methods: The Finnvasc registry included data on 3,925 infrainguinal surgical revascularization procedures. This database was randomly divided into a derivation and a validation data set of similar sizes.

Adjuvant arteriovenous fistula as means of rescue for infrapopliteal venous bypass with poor runoff.

Objective: The aim of this study was to assess the outcome of infrapopliteal bypass when an adjuvant arteriovenous (AV) fistula was reconstructed as means of rescue as a result of poor runoff. The design was a retrospective multicenter case-control study.

Methods: Seventy-seven infrapopliteal vein bypasses required an adjuvant AV fistula among 1813 patients operated on for critical leg ischemia in 3 vascular centers between 1996 and 2003.

Crystal structures of the catalytic domain of phosphodiesterase 4B complexed with AMP, 8-Br-AMP, and rolipram.

Phosphodiesterase catalyzes the hydrolysis of the intracellular second messenger 3',5'-cyclic AMP (cAMP) into the corresponding 5'-nucleotide. Phosphodiesterase 4 (PDE4), the major cAMP-specific PDE in inflammatory and immune cells, is an attractive target for the treatment of asthma and COPD. We have determined crystal structures of the catalytic domain of PDE4B complexed with AMP (2.

Urokinase, tissue-type plasminogen activator and plasminogen activator inhibitor-1 expression in severely stenosed and occluded vein grafts with thrombosis.

Intimal hyperplasia and subsequent thrombotic occlusions limit the success of vascular reconstructive procedures. Plasminogen activation in situ may be an important factor affecting re-stenosis of the graft. Tissue specimens from eight patients with failing or failed infra-inguinal vein bypasses and three specimens from normal veins were harvested to study urokinase-type plasminogen activator (u-PA), tissue-type plasminogen activator (t-PA) and plasminogen activator inhibitor-1 (PAI-1) by in situ hybridization and immunohistochemistry.