A Review on the Antitumor Activity of Various Nitrogenous-based Heterocyclic Compounds as NSCLC Inhibitors.

At present, cancers have been causing deadly fears to humans and previously unpredictable losses to health. Especially, lung cancer is one of the most common causes of cancer-related mortality accounting for approximately 15% of all cancer cases worldwide. While Non-Small Cell Lung Carcinomas (NSCLCs) makes up to 80% of lung cancer cases.

Synthesis and Antimicrobial Evaluation of (Z)-5-((3-phenyl-1H-pyrazol-4- yl)methylene)-2-thioxothiazolidin-4-one Derivatives.

Background: An alarming increment in pathogenic resistance to existing anti-microbial agents is a serious problem and the treatment of these bacterial infections is becoming increasingly challenging. Therefore, there is an urgent need to develop novel antimicrobial agents.

Objective: As a part of our ongoing studies toward the development of novel antibacterial agents, the synthesis and antibacterial activity of a series of (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives will be discussed in this study.

Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.

Three series of 1,3-diaryl pyrazole derivatives bearing aminoguanidine or furan-2-carbohydrazide moieties have been synthesized, characterized and evaluated for antibacterial and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1-64 μg/mL. Compounds 6g, 6l and 7l presented the most potent inhibitory activity against Gram-positive bacteria (e.

Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.

Three series of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety (5a-k, 6a-i, and 7a-i) have been synthesized, characterized and evaluated for their antibacterial activity. Some of these displayed potent antibacterial activity against several Gram-positive and Gram-negative bacterial strains (including multidrug-resistant clinical isolates) with minimum inhibitory concentration (MIC) values in the range of 4-64 μg/mL and minimum bactericidal concentration (MBC) values in the range of 8-256 μg/mL. Compared with previously reported rhodanine derivatives, these compounds exhibited a broad spectrum of antibacterial activity by means of introducing 4-amino-5-aryl-1,2,4-triazole-3-thione moiety.

Synthesis and positive inotropic evaluation of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted piperazine moieties.

Four series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted piperazine moieties were synthesized and evaluated for their positive inotropic activity by measuring the left atrium stroke volume in isolated rabbit-heart preparations. Several compounds were developed and showed favorable activities compared to the standard drug milrinone, with (4-([1,2,4]triazolo[3,4-a]phthalazin-6-yl)piperazin-1-yl)(p-tolyl)methanone (5g) being identified as the most potent with an increased stroke volume of 19.15±0.

Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.

Two novel series of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives were designed and synthesized, and their anti-bacterial activities evaluated. These compounds showed broad-spectrum inhibitory activities against both Gram-positive and Gram-negative bacteria with minimum inhibitory concentration (MIC) values in the range of 1-64 μg/mL. The activity of compound 6c was the more potent with MIC values of 1 μg/mL against the MRSA (3167 and 3506) strains than those of gatifloxacin, oxacillin, and norfloxacin.

[Research on the relationship between levels of soluble cluster of differentiation 40 ligand, matrix metalloproteinase 9 and pregnancy-associated plasma protein A in serum and stability of carotid plaques].

Objectives: To study the relationship between serum levels of some inflammatory markers and stability of carotid plaques in the patients with carotid plaques and evaluate the ability of each serum marker in identifying vulnerable carotid plaques.

Methods: The study included 65 consecutive patients with carotid plaques confirmed by imaging examinations from March 2008 to March 2010. All the patients were classified as stable plaques group (n = 21) and unstable plaques group (n = 44) according to the characteristic findings of the plaques in MRI such as the thickness of fibrous cap, the existence of large lipid core and the intra-plaque hemorrhage.

Tiny intracranial aneurysms: endovascular treatment by coil embolisation or sole stent deployment.

Purpose: Tiny intracranial aneurysms pose a significant therapeutic challenge for interventional neuroradiologists. The authors report their preliminary results of endovascular treatment of these aneurysms.

Methods: Between January 2002 and December 2009, 52 tiny intracranial aneurysms (defined as ≤ 3 mm in maximum diameter) in 46 patients (22 men; mean age, 57.

[Endovascular management of symptomatic carotid stenosis combined with kinking].

Objective: To study the necessity, feasibility, security of carotid angioplasty and stenting (CAS) for symptomatic carotid stenosis combined with kinking.

Methods: Twelve patients with symptomatic carotid stenosis and kinking demonstrated by digital subtraction angiography (DSA) received CAS from December 2003 to December 2009. There were 9 male and 3 female patients, age ranged from 59 to 77 years (mean 69.

[Endovascular treatment of micro-intracranial aneurysms: adverse factors of micro-catheterization and its relevant managements].

Objectives: To investigate adverse factors that may hinder successful placement and stabilization of the microcatheter during endovascular therapy of micro-intracranial aneurysms (≤ 3 mm in maximum diameter), and to explore the relevant managements.

Methods: Forty-six patients with fifty-one micro-intracranial aneurysms treated by endovascular therapy from June 2001 to October 2009 were retrospectively analyzed for their intervention data.

Results: Adverse factors of optimal micro-catheterization mainly included, tortuosity of the proximal vessels (PVs) and the parent artery (PA), relative large gap in diameter among the PVs, the PA and the microcatheter, relative large divergence in direction among the PVs, the PA and the aneurysm dome, and stent deployed in the PA.

[Endovascular treatment of ruptured and unruptured intracranial very small aneurysms].

Objective: To evaluate the feasibility and safety of endovascular treatment of ruptured and unruptured intracranial very small aneurysms (< or = 3 mm in maximal diameter).

Methods: Forty-eight intracranial very small aneurysms in 44 patients treated with endovascular therapy from June 2001 to August 2009 were reviewed retrospectively in clinical, imaging, interventional and follow-up data. Among 44 patients, there were 20 males and 24 females with a mean age of 57.

[Changes of nitric oxide and endothelin serum level after carotid balloon denudation or stent assisted angioplasty: an experimental and clinical observation].

Objective: To observe the changes of nitric oxide (NO) and endothelin (ET) serum level in the Guangxi BA-MA minipigs whose carotid arteries were injured by balloon denudation and in the patients with carotid stent assisted angioplasty.

Methods: Twelve Guangxi BA-MA minipigs were chosen. High fat/cholesterol feeding and endovascular balloon denudation were used to create a carotid artery atherosclerotic stenosis animal model.

[Evaluation of cerebral hemodynamics in geriatric carotid stenosis pre- and post-carotid artery stenting].

Objectives: To explore influencing factors of regional cerebral blood flow (rCBF) in geriatric carotid stenosis, and to analyze changes of rCBF and clinical symptoms after carotid stenting.

Methods: During August 2005 and April 2008, 68 geriatric patients of carotid stenosis having SPECT examination in our hospital were retrospectively studied, whose diagnosis was approved by angiography. Correlated rCBF was compared separately in different stenotic degrees of carotid stenosis, in unilateral or bilateral stenosis, accompanied with vertebrobasilar stenosis (VBS) or not, with collateral circulation or not, before and after carotid stenting.

[Effect of different duration of clopidogrel pretreatment on platelet activation in patients undergoing stenting].

Objective: To investigate the effect of two clopidogrel pretreatment duration on platelet activation in patients undergoing stenting.

Methods: From July 2006 to December 2007 40 elective carotid or vertebral artery stenting patients were assigned into two groups: Group A (n = 24) initiated clopidogrel (75 mg/d) > or = 5 d before stenting; group B (n = 16) initiated 3 - 4 days. Platelet-monocyte aggregates and fibrinogen receptors analyzed by flow cytometric, and platelet aggregation tests using optical aggregometry, as well as serum soluble CD40 ligand quantified by enzyme-linked immunosorbent assay were assessed in peripheral blood samples obtained immediately before and at 0.

[Clinical study and numerical simulation of hemodynamics in the tortuosity of internal carotid artery].

Objectives: To establish a theoretical model for the tortuosity of internal carotid artery and summarize the hemodynamic rule of blood flow in a tortuous artery. To explore the relationship of cerebral ischemia and tortuous internal carotid artery.

Methods: Taking the internal carotid artery as a prototype, a geometric model of a tortuous artery was constructed according to the normal physiological and anatomical parameters of internal carotid artery.

[Treatment of spinal cord hemangioblastoma by microoperations combined with embolization].

Objective: To investigate the effects of microoperations combined with embolization in treatment of spinal cord hemangioblastoma.

Methods: Thirty-six patients with spinal cord hemangioblastoma, 21 males and 15 females, aged 24.2 (12-48), underwent MRI and digital abstraction angiography.

Serial changes of circulating platelet activation markers after carotid artery stenting.

We investigated serial changes of circulation platelet activation markers in 40 patients undergoing carotid artery stenting under the protection of dual antiplatelet therapy and filter devices. Monocyte-platelet aggregates and PAC-1 (a marker specific for activated glycoprotein IIb/IIIa) analyzed by flow cytometry were determined in patients with symptomatic stenosis undergoing elective carotid artery stenting. Blood samples were obtained immediately before stent implantation and 0.

Treatment of patients older than 60 years with symptomatic vertebrobasilar artery stenosis.

Background: Vertebrobasilar artery stenosis is an important cause of ischemic posterior circulation strokes. This study aimed at evaluating the safety and efficacy of treatment including conservative therapy alone and conservative plus endovascular therapy for elderly patients with symptomatic vertebrobasilar artery stenosis.

Methods: Patients older than 60 years with symptomatic vertebrobasilar artery stenosis (> or = 50%) confirmed by cerebral angiography were enrolled.

[Management of elderly patients with symptomatic vertebrobasilar insufficiency].

Objective: To evaluate the feasibility, safety and short-term efficacy of stent-assisted angioplasty and/or drug therapy for elderly patients with symptomatic vertebrobasilar insufficiency.

Methods: Elderly patients (> or = 60 years old) with symptomatic vertebrobasilar stenosis (> or = 50%) demonstrated by cerebral angiography were treated with drug therapy and some with endovascular stenting further from April 2001 to June 2006. The clinical, imaging, intervention and follow-up data were collected and analyzed.