Abstract：
AIM:To develop potent HIF-1α inhibitors for potential treatment of cancer. MATERIALS AND METHODS:Chemical synthesis, HIF-luciferase assay, cytotoxic assay, platelet aggregation assay, western blot analysis, quantitative real-time PCR, aqueous solubility, protein binding, metabolic stability, and metabolic pathways. RESULTS:Thirteen novel benzimidazole analogs were synthesized. Compounds 3a and 3k showed the highest anti-HIF-1α activity. They are significantly more effective than YC-1 in the suppression of HIF-1α protein expression based on western blot assay. They show comparable potency in inhibition of cancer cell migration. They are less potent in the inhibition of platelet aggregation. 3k had the most favorable drug-like properties, including long half-life in human liver microsomes, medium protein binding level and reasonable aqueous solubility. CONCLUSION:The potent anti-HIF-1α activity and favorable drug-like properties of compound 3k suggest that it may hold great potential as an adjuvant therapy for cancer treatment through repression of HIF-1α protein expression.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Chen J,Wang J,Schwab LP,Park KT,Seagroves TN,Jennings LK,Miller DD,Li Wsubject
Has Abstractpub_date
2014-08-01 00:00:00pages
3891-904issue
8eissn
0250-7005issn
1791-7530pii
34/8/3891journal_volume
34pub_type
杂志文章abstract：:Allelic loss at specific chromosomal loci was demonstrated in carcinoma of the cervix (CaCx) obtained from Hong Kong Chinese by restriction fragment length polymorphism analysis. Altogether 12 patients with CaCx, 7 with cervical intraepithelial neoplasia (CIN) and 7 with normal cervical tissues were studied. Polymorph...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1992-09-01 00:00:00
abstract：BACKGROUND:Inhibition of the vascular endothelial growth factor receptor (VEGFR) has been shown to improve the radiation response of several experimental tumors. The present experimental study compares the effect of neoadjuvant, concomitant and adjuvant treatment with PTK787/ZK222584, a specific inhibitor of the VEGFR,...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2003-09-01 00:00:00
abstract：BACKGROUND:The long-term goal of this work is to develop a new therapeutic regimen for the treatment of colon cancer in humans which will include hyperthermic intraperitoneal perfusion of verapamil as an alternative to administration of chemotherapy. METHODS AND RESULTS:Hyperthermia and verapamil caused a significant ...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1997-05-01 00:00:00
abstract：BACKGROUND:Intradermal or oral administration of lipopolysaccharide derived from Pantoea agglomerans (IP-PA1) has shown prophylactic and antitumor effects without serious side-effects. While it is known that tumor necrosis factor (TNF)-alpha produced by activated macrophages plays an important role in the expression me...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2009-11-01 00:00:00
abstract：:The most widely-known anti-tumor drugs often induce marked immunosuppression which can give rise to one or more sepses. Anti-infection measures immediately applied can sometimes prove largely ineffective or even useless, the patient dying not as a result of the spread of the tumour but as a direct consequence of oppor...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1997-11-01 00:00:00
abstract：:Within the brain, dissemination of glioma cells follows myelinated fiber tracts and extracellular matrix containing structures such as the basement membranes of blood vessels. These patterns represent the two major routes of invasion frequently observed in clinical disease. Previously, we have characterized the substr...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1998-07-01 00:00:00
abstract：:Menogaril is an antitumor agent active after oral administration, and unlike other anthracyclines, extravasation cannot occur. When the IC90 values of menogaril were plotted versus exposure time on a double-logarithmic scale, the regression lines had slopes between -0.64 and -0.80. These results showed that the mode o...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1996-09-01 00:00:00
abstract：:Glioblastoma multiforme (GBM) represents the most malignant primary brain tumor in adults with generally dismal prognosis, early clinical deterioration and high mortality. GBM is extremely invasive, characterized by intense and aberrant vascularization and high resistance to multimodal treatment. Standard therapy (sur...
journal_title：Anticancer research
pub_type： 杂志文章,评审
doi：10.21873/anticanres.11285
更新日期：2017-01-01 00:00:00
abstract：:Gynaecologic oncology day surgery deals primarily with the diagnosis of endometrial, cervical, vulvar and vaginal tumors. Conscious sedation is an important technique used in gynaecologic oncology day surgery. It is often associated with regional anaesthesia. The goals of conscious sedation are to provide effective pa...
journal_title：Anticancer research
pub_type： 临床试验,杂志文章,随机对照试验
doi：
更新日期：2004-11-01 00:00:00
abstract：BACKGROUND:It has been suggested that prognosis in familial breast cancer could be influenced by the parent of origin, with a worse prognosis when inherited paternally. This study aimed to investigate the effect of the parent of origin on prognosis. PATIENTS AND METHODS:Index patients were divided into two study group...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.11442
更新日期：2017-03-01 00:00:00
abstract：BACKGROUND/AIM:Although insulin-like growth factor-1 (IGF-1) is well-implicated in cancer biology, the potential roles of IGF-1 variants in different types of cancer are largely unknown. The aim of the present study was to in vitro characterize several human cancers for their IGF-1 variant expression patterns. MATERIA...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2015-01-01 00:00:00
abstract：:Tumor cell invasion was studied using the 9-day chick embryo skin (CES). The invasion process was broken down into 4 sequential events: adhesion, penetration, proliferation and colonization. Tumor cells used in this study included cells from various human and canine solid tumors, tumor cell lines from human and animal...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1989-01-01 00:00:00
abstract：:We have previously described that thymic lymphomas from anti HY-TCR transgenic mice were resistant to TCR-induced (calcium-mediated) apoptosis but sensitive to induction of apoptosis by etoposide. A defect of apoptosis in these cells is located downstream of the nuclear receptor Nur77 induction and upstream from the e...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2003-03-01 00:00:00
abstract：BACKGROUND/AIM:Anthracyclines, such as doxorubicin, though widely used in anticancer therapy, they are associated with cardiotoxic side-effects. The aim of this trial was to investigate long-term follow-up cardiotoxicity findings in patients treated with doxorubicin and concomitant metoprolol or enalapril 10 years earl...
journal_title：Anticancer research
pub_type： 杂志文章,随机对照试验
doi：10.21873/anticanres.13769
更新日期：2019-10-01 00:00:00
abstract：:The polysaccharide produced by the red microalga Porphyridium sp. was highly inhibitory for cell transformation of mouse fibroblast cells by an MSV-124 virus stock. This inhibition was most effective if the polysaccharide was added 2 h before or at the time of infection. The finding that the inhibition of cell transfo...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2001-05-01 00:00:00
abstract：BACKGROUND:Genetic polymorphisms of carcinogen-metabolizing enzyme genes have been associated with the risk of oral squamous cell carcinoma and oral leukoplakia. The overexpression of p53 protein is the most common genetic alteration in head and neck cancer. In the present study the combined or isolated presence of glu...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2008-03-01 00:00:00
abstract：:5-Fluorouracil (5FU) increases the rate of incorporation of tritiated thymidine (3HTdR) and iododeoxyuridine (125 IUdR) into the cell and its DNA. 5FU has differential effect on metabolism of DNA through its specific action on thymidylate synthetase. Effects of 5FU on the incorporation of other metabolic precursors we...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1982-05-01 00:00:00
abstract：BACKGROUND:As a majority of ovarian cancer patients will ultimately develop recurrent disease, there is an urgent need for alternative or additional approaches in the treatment of this cancer. MATERIALS AND METHODS:The antitumour effect of i.p. administered cisplatin, liposomal muramyltripeptide phosphatidylethanulami...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2000-07-01 00:00:00
abstract：:The purpose of this study was to determine whether the degree of anchorage-independent growth of rodent or human cells in increasing concentrations of agarose correlated with successful transfection of the cells with an activated c-Ha-ras oncogene and tumorigenicity in nude mice. NIH 3T3 cells, C3H 10T1/2 fibroblasts,...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1991-01-01 00:00:00
abstract：BACKGROUND:This case report describes a patient with symptomatic anaemia due to a bleeding duodenal metastasis from metastasising differentiated thyroid cancer (DTC), which was treated by partial duodenopancreatectomy (DP). CASE REPORT:A 71-year old male was sent to hospital with severe anaemia. This patient had suffe...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2006-05-01 00:00:00
abstract：:We studied 19 patients, 12 males and 7 females of a median age of 49 years (range 26-76) with clinical manifestations of gastro-intestinal (GI) involvement from malignant melanoma. Their records were available from an electronic database of 2163 patients registered between 1977 and 1998 with the Melanoma Unit initiall...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2001-03-01 00:00:00
abstract：BACKGROUND/AIM:To study the changes of glioblastoma multiforme during chemoradiotherapy (CRT) and to evaluate the impact of changes on dosimetry and clinical outcomes. PATIENTS AND METHODS:Forty-three patients underwent volumetric imaging-based replanning. Prognostic factors and gross tumor volume changes in relation ...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.14425
更新日期：2020-08-01 00:00:00
abstract：AIM:This study assessed the symptoms and health-related quality of life (HRQOL) of patients with advanced non-small cell lung cancer (NSCLC) and examined the symptom-associated characteristics. PATIENTS AND METHODS:The symptoms of 122 patients with NSCLC scheduled for chemotherapy before starting treatment were survey...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2016-08-01 00:00:00
abstract：:The expression of p53 and mdm-2 proteins was analysed in parrafin sections from 39 cases of Hodgkin's disease (HD) and compared to the presence of Epstein-Barr Virus (EBV). P53 protein was found in Hodgkin and Reed-Sternberg (HRS) cells in 12/39 cases. Mdm-2 protein was found in HRS cells in 10/39 cases. EBV-encoded E...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1996-09-01 00:00:00
abstract：AIM:The current study aimed to determine the prognostic significance of thrombocytosis in patients with colorectal cancer (CRC) by a meta-analysis of the literature. PATIENTS AND METHODS:The meta-analysis followed the 2009 guidelines of Preferred Reporting Items for Systematic Reviews and Meta-Analyses. A systematic l...
journal_title：Anticancer research
pub_type： 杂志文章,meta分析,评审
doi：10.21873/anticanres.11878
更新日期：2017-09-01 00:00:00
abstract：BACKGROUND:Screening gastroscopic examinations were performed in a cohort of individuals at high risk for developing gastric carcinoma (GC). PATIENTS AND METHODS:Five gastric biopsies were obtained following the Houston schema. Five histological parameters of gastritis were investigated: acute gastritis, chronic gastr...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2012-05-01 00:00:00
abstract：UNLABELLED:The aim of this study was to evaluate the efficacy and safety of erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in Japanese patients with relapsed or recurrent advanced non-small cell lung cancer (NSCLC). PATIENTS AND METHODS:This was a multicentre, open-label phase II study of er...
journal_title：Anticancer research
pub_type： 杂志文章,多中心研究
doi：
更新日期：2010-02-01 00:00:00
abstract：BACKGROUND/AIM:Individualized proper chemotherapy using in vitro drug sensitivity testing has been proposed as a novel therapeutic modality and shown to have better efficacy than empiric chemotherapy. However, issues around establishing a patient-derived cell culture or xenograft, the timing of the testing obtained, an...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.13920
更新日期：2019-12-01 00:00:00
abstract：BACKGROUND/AIM:Since the first description of five pericytomas with the t(7;12)/ACTB-GLI1 fusion gene, only three new tumors were studied by both cytogenetics and molecular techniques. We report here genetic data on another case of this rare tumor. MATERIALS AND METHODS:Cytogenetic, fluorescence in situ hybridization ...
journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.14065
更新日期：2020-03-01 00:00:00
abstract：AIM:The suitability of Papanicolaou staining and of hematoxylin staining for DNA single-cell cytometry was investigated in comparison to Feulgen staining. MATERIALS AND METHODS:Ten normal cervical smears and ten cervical smears containing cells of a squamous cell carcinoma in situ were analyzed. The integrated optical...
journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2011-01-01 00:00:00
