Exploring the Biological Activity of a Library of 1,2,5-Oxadiazole Derivatives Endowed With Antiproliferative Activity.

Abstract:

BACKGROUND/AIM:The identification of a series of oxadiazole-based compounds, as promising antiproliferative agents, has been previously reported. The aim of this study was to explore the SAR of newly-synthesized oxadiazole derivatives and identify their molecular targets. MATERIALS AND METHODS:A small library of 1,2,5-oxadiazole derivatives was synthetized and their antiproliferative activity was tested by the MTT assay. Their interaction with topoisomerase I was evaluated and a molecular docking study was performed. RESULTS:Several candidates showed cytotoxicity towards two human tumor cell lines, HCT-116 (colorectal carcinoma) and HeLa (cervix adenocarcinoma). Some derivatives exhibited inhibitory effects on the catalytic activity of topoisomerase I and this effect was supported by docking studies. CONCLUSION:The enzyme inhibition results, although not directly related to cytotoxicity, suggest that a properly modified 1,2,5 oxadiazole scaffold could be considered for the development of new anti-topoisomerase agents.

journal_name

Anticancer Res

journal_title

Anticancer research

authors

Gelain A,Mori M,Meneghetti F,Porta F,Basile L,Marverti G,Asai A,Hyeraci M,García-Argáez AN,Via LD,Guccione S,Villa S

doi

10.21873/anticanres.13089

subject

Has Abstract

pub_date

2019-01-01 00:00:00

pages

135-144

issue

1

eissn

0250-7005

issn

1791-7530

pii

39/1/135

journal_volume

39

pub_type

杂志文章
  • Signal pathways involved in apigenin inhibition of growth and induction of apoptosis of human anaplastic thyroid cancer cells (ARO).

    abstract::Recently we demonstrated that several flavonoids can inhibit the proliferation of certain human thyroid cancer cell lines. Among the flavonoids tested, apigenin and luteolin are the most effective inhibitors of these tumor cell lines. In the present study, we investigated the signal transduction mechanism associated w...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Yin F,Giuliano AE,Van Herle AJ

    更新日期:1999-09-01 00:00:00

  • Infusion pharmacokinetics of Lipocurc™ (liposomal curcumin) and its metabolite tetrahydrocurcumin in Beagle dogs.

    abstract::Curcumin's instability and its metabolite, tetrahydrocurcumin (THC) pose a major issue for the establishment of dependable pharmacokinetics and excretion profiles. Additional pharmacokinetic variances are associated with durations of intravenous infusions. We found that stabilizing curcumin with phosphoric acid allows...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Helson L,Bolger G,Majeed M,Vcelar B,Pucaj K,Matabudul D

    更新日期:2012-10-01 00:00:00

  • Cysteine proteinase inhibitors reduce malignant melanoma cell invasion in vitro.

    abstract::Proteolytic enzymes are believed to be necessary for tumor cell invasion. We have studied the effects of the cysteine proteinase inhibitor E-64 and the serine and cysteine proteinase inhibitor leupeptin, on the ability of human malignant melanoma cells (LOX) to pass through an artificial basement membrane. Transwell c...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Bjørnland K,Buø L,Kjønniksen I,Larsen M,Fodstad O,Johansen HT,Aasen AO

    更新日期:1996-07-01 00:00:00

  • Detection of oncogenic HPV and identification of 72Arg polymorphic p53 by in situ PCR for clinical routine purposes.

    abstract:BACKGROUND:Ano-genital carcinoma is a polyfactorial and polygenic disease. Certain strains of human papillomavirus (HPV) have been detected in a high percentage of patients. It has been suggested that p53 polymorphisms may be relevant for the interaction with viral proteins that inactivates p53. MATERIALS AND METHODS:...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Realacci M,Perrone GA,Sale P,Tafani M,Di Vito M,Perrone-Donnorso R,Zotti G,Russo MA

    更新日期:2006-07-01 00:00:00

  • Glioma cell adhesion and migration on human brain sections.

    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:

    authors: Giese A,Laube B,Zapf S,Mangold U,Westphal M

    更新日期:1998-07-01 00:00:00

  • Visualization of the metastatic process by green fluorescent protein expression.

    abstract::We demonstrate here the visualization of the cancer metastatic process in live tissue in vivo by green fluorescent protein (GFP) expression. The human lung adenocarcinoma cell-line Anip 973 was transfected with the humanized GFP-S65T cDNA and stable high-level GFP-expressing transfectants were established. GFP transfe...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Chishima T,Miyagi Y,Wang X,Tan Y,Shimada H,Moossa A,Hoffman RM

    更新日期:1997-07-01 00:00:00

  • Expression of several resistance mechanisms in untreated human kidney and lung carcinomas.

    abstract::Thirty human renal cell carcinomas and 94 non-small cell lung carcinomas of previously untreated patients were analyzed for the presence of P-glycoprotein, glutathione S-transferase-pi and topoisomerase II by means of immunohistochemistry. In the renal cell carcinomas investigated, two resistance markers were seen in ...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Volm M,Mattern J,Efferth T,Pommerenke EW

    更新日期:1992-07-01 00:00:00

  • Outcomes of Laparoscopic Surgery in Colorectal Cancer Patients With Dialysis.

    abstract:BACKGROUND/AIM:To investigate the outcomes of laparoscopic surgery in colorectal cancer patients with dialysis. PATIENTS AND METHODS:Fourteen dialysis (dialysis group) and 567 non-dialysis (non-dialysis group) patients who underwent laparoscopic and open surgery for colorectal cancer between April 2008 and December 20...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.14176

    authors: Higashino N,Matsuda T,Hasegawa H,Yamashita K,Sakamoto H,Fujikawa M,Yamamoto M,Kanaji S,Oshikiri T,Nakamura T,Suzuki S,Kakeji Y

    更新日期:2020-04-01 00:00:00

  • Comparison of Cold Atmospheric Plasma Devices' Efficacy on Osteosarcoma and Fibroblastic In Vitro Cell Models.

    abstract:BACKGROUND/AIM:Cold atmospheric plasma (CAP) attenuates tumor cell proliferation and induces apoptosis in various cell lines. While exerting marginal effects on non-neoplastic cells this unfolds promising applications in cancer therapy. The aim of the study was to analyse the effects of different CAP sources and applic...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.11968

    authors: Gümbel D,Suchy B,Wien L,Gelbrich N,Napp M,Kramer A,Ekkernkamp A,Daeschlein G,Stope MB

    更新日期:2017-10-01 00:00:00

  • Radiotherapy as Definitive Treatment of Patients with Primary Vulvar Carcinoma Unfit for Surgery and with Recurrent Vulvar Carcinoma After Primary Radical Surgery: Results of a Retrospective Single-center Study.

    abstract:AIM:To assess the outcome of patients with vulvar carcinoma unfit for surgery treated with radiotherapy for primary disease and for those with recurrent disease after primary surgery. PATIENTS AND METHODS:The study was conducted on 16 patients with primary disease and 31 with recurrent disease. RESULTS:An objective r...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Laliscia C,Gadducci A,Montrone S,Tana R,Morganti R,Fabrini MG

    更新日期:2016-01-01 00:00:00

  • Cell culture as spheroids: an approach to multicellular resistance.

    abstract::Cells cultured as spheroids present an heterogeneity similar to that of tumours in vivo. In the spheroid peripheral layers, cells are proliferating, deeper cells are non-cycling, when in the aggregate centre, cells form often a necrotic core. A multicellular resistance is related on the cell contact to other cells or ...

    journal_title:Anticancer research

    pub_type: 杂志文章,评审

    doi:

    authors: Desoize B,Gimonet D,Jardiller JC

    更新日期:1998-11-01 00:00:00

  • Ascorbic acid induces either differentiation or apoptosis in MG-63 osteosarcoma lineage.

    abstract:BACKGROUND/AIM:Osteosarcoma originates from mesenchymal stem cells with impaired bone differentiation. In the present study we investigated the effect of ascorbic acid (AsA) on osteogenic differentiation and apoptosis of the MG-63 osteosarcoma cell line. MATERIALS AND METHODS:We evaluated the expression of runt-relate...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Valenti MT,Zanatta M,Donatelli L,Viviano G,Cavallini C,Scupoli MT,Dalle Carbonare L

    更新日期:2014-04-01 00:00:00

  • Effect of Fibroblast Growth Factor-2 and its Receptor Gene Polymorphisms on the Survival of Patients With Hepatitis B Virus-associated Hepatocellular Carcinoma.

    abstract:BACKGROUND/AIM:Fibroblast growth factor (FGF), vascular endothelial growth factor, and hepatocyte growth factor play a critical role in the pathogenesis of hepatocellular carcinoma (HCC). MATERIALS AND METHODS:We assessed nine single nucleotide polymorphisms (SNPs) in the FGF1, FGF2, FGF receptor (FGFR)-2, Flt-1, and ...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.13337

    authors: Kim SS,Eun JW,Cho HJ,Lee HY,Seo CW,Noh CK,Shin SJ,Lee KM,Cho SW,Cheong JY

    更新日期:2019-04-01 00:00:00

  • Ex vivo evaluation of a bipolar application concept for radiofrequency ablation.

    abstract:BACKGROUND:Bipolar radiofrequency ablation (RFA) can avoid complications such as thermal tissue damage, a possible consequence of monopolar RFA. However, basic studies about the dosage/effect relationship of bipolar systems are missing. This is systematic research on ex vivo beef livers to find which capacity parameter...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Zurbuchen U,Frericks B,Roggan A,Lehmann K,Bössenroth D,Buhr HJ,Ritz JP

    更新日期:2009-04-01 00:00:00

  • Immunosuppression Induced by Perioperative Peritonitis Promotes Lung Metastasis.

    abstract:BACKGROUND/AIM:Perioperative intra-abdominal infection has been reported as a risk factor for metastasis. The aim of this study was to investigate the mechanism by which peritonitis induces immunosuppression in the lung, which in turn promotes lung metastasis. MATERIALS AND METHODS:C57BL/6 mice were intravenously admi...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.12733

    authors: Arimoto A,Yamashita K,Hasegawa H,Sugita Y,Fukuoka E,Tanaka T,Suzuki S,Kakeji Y

    更新日期:2018-07-01 00:00:00

  • Aberrant methylation of the UNC5C gene is frequently detected in advanced colorectal cancer.

    abstract:BACKGROUND:UNC5C, one of the Netrin-1 receptors, belongs to the functional dependence receptor family, members of which share the ability to induce apoptosis in the absence of their ligands. Recently, two reports indicated that UNC5C methylation was closely associated with loss of gene expression in colorectal cancer. ...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Hibi K,Mizukami H,Shirahata A,Goto T,Sakata M,Saito M,Ishibashi K,Kigawa G,Nemoto H,Sanada Y

    更新日期:2009-01-01 00:00:00

  • DNA-dependent protein kinase in leukaemia cells and correlation with drug sensitivity.

    abstract::We investigated whether the levels of the DNA-dependent protein kinase (DNA-PK) activity and content correlate with drug sensitivity in different tumour materials and if this can be utilised in predicting treatment outcome. DNA-PK activity and expression were investigated in tumour cells from 8 patients with chronic l...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Eriksson A,Lewensoh R,Larsson R,Nilsson A

    更新日期:2002-05-01 00:00:00

  • Prognostic Significance of Solid and Micropapillary Components in Invasive Lung Adenocarcinomas Measuring ≤3 cm.

    abstract:BACKGROUND/AIM:We aimed to analyze the clinical impact of solid and micropapillary components in a series of Japanese patients resected for ≤3 cm lung adenocarcinoma. PATIENTS AND METHODS:A total of 115 patients with ≤3 cm lung adenocarcinomas were reviewed and classified according to the American Thoracic Society and...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.11058

    authors: Matsuoka Y,Yurugi Y,Takagi Y,Wakahara M,Kubouchi Y,Sakabe T,Haruki T,Araki K,Taniguchi Y,Nakamura H,Umekita Y

    更新日期:2016-09-01 00:00:00

  • Potentiation by dipyridamole of 5-fluorouridine antitumor activity against a rat adenocarcinoma in vivo.

    abstract::Rats were inoculated subcutaneously into both flanks with a transplantable adenocarcinoma of the colon. They were treated intravenously with either 5-FUrd (5-fluorouridine) or 5-FdUrd (5-fluoro-2'-deoxyuridine) with or without addition of dipyridamole 20 and 30 min later, respectively, for 3 consecutive days. Dipyrida...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: el Hag IA,Roos G,Jönsson PE,Stenram U

    更新日期:1990-01-01 00:00:00

  • Expression of ATP-binding Cassette Transporter 11 (ABCC11) Protein in Colon Cancer.

    abstract:AIM:To investigate the clinical significance of ATP-binding cassette transporter 11 (ABCC11) protein expression in colon cancer. MATERIALS AND METHODS:One hundred thirty nine patients with colon cancer resection between 2009 and 2011 were enrolled. The relationship with immunohistochemical ABCC11 staining and clinicop...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.14549

    authors: Yamada Y,Yoshimatsu K,Yokomizo H,Okayama S,Shiozawa S

    更新日期:2020-10-01 00:00:00

  • The Tumor-promoting Effects of FAM92A1-289 in Cervical Carcinoma Cells.

    abstract:BACKGROUND/AIM:FAM92A1-289 is recognized as one of the newly-discovered putative oncogenes. This study was performed to reveal its oncogenic functions in human cervical carcinoma cells. MATERIALS AND METHODS:The FAM92A1-289+ cell line was established with knock-in technique and selected by puromycin-resistance screeni...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.11090

    authors: Gui H,Guo XR,Fang J,Ma SN,Wu G,Shen JH,Tu HJ,Li DS,Dai LJ,Ruan XZ

    更新日期:2016-10-01 00:00:00

  • Lonidamine-induced outer membrane permeability and susceptibility of mitochondria to inhibition by adriamycin.

    abstract::Low concentrations of Adriamycin (ADM) do not inhibit the oxygen consumption of rat liver mitochondria because of the inability to cross the outer membrane. The involvement of this membrane as a permeability barrier is demonstrated by the results with exogenous ferrocytochrome c. ADM does not affect the basal rate of ...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Floridi A,Bianchi C,Bagnato A,Gambacurta A,Paggi MG,Silvestrini B,Caputo A

    更新日期:1987-11-01 00:00:00

  • Overexpression of tissue inhibitor of metalloproteinase-1 gene correlates with poor outcomes in colorectal cancer.

    abstract::Tissue inhibitor of metalloproteinase-1 (TIMP-1) is a major endogenous regulator of matrix metalloproteinases. This study examined the relation between TIMP-1 gene expression and postoperative mortality in patients with colorectal cancer (CRC). Specimens of CRC were obtained from 202 patients. The relative expression ...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Inagaki D,Oshima T,Yoshihara K,Tamura S,Kanazawa A,Yamada T,Yamamoto N,Sato T,Shiozawa M,Morinaga S,Akaike M,Fujii S,Numata K,Kunisaki C,Rino Y,Tanaka K,Masuda M,Imada T

    更新日期:2010-10-01 00:00:00

  • Cyclooxygenase-2 expression in human soft-tissue sarcomas is related to epithelial differentation.

    abstract:BACKGROUND:Cyclooxygenase-2 (Cox-2) is expressed by several types of epithelial malignancies, i.e., carcinomas, and inhibition of Cox-2 may have a therapeutic role in chemoprevention and treatment of cancer. The role of Cox-2 in non-epithelial malignancies, however, is unclear. MATERIALS AND METHODS:We investigated, b...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Lassus P,Ristimäki A,Huuhtanen R,Tukiainen E,Asko-Seljavaara S,Andersson LC,Miettinen M,Blomqvist C,Haglund C,Böhling T

    更新日期:2005-07-01 00:00:00

  • Adenocarcinoma production in rats administered 1,2-dimethylhydrazine and fed iron salt and guar gum diets.

    abstract::Iron salts supplemented in a basal ratio, were fed to young Sprague-Dawley male rats for prolonged periods and the frequency of colonic adenocarcinomas induced by repeated s.c. injection of 1,2-dimethylhydrazine (DMH) at unit base doses of 9.0 mg/kg, ascertained and compared with the respective controls. In a series e...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Gershbein LL,Rezai VK,Amir-Mokri E,Rao KC

    更新日期:1993-11-01 00:00:00

  • Vitamin D and Myofibroblasts in Fibrosis and Cancer: At Cross-purposes with TGF-β/SMAD Signaling.

    abstract::The multifaceted involvement of the active vitamin D metabolite 1,25-dihydroxyvitamin D3 (henceforth referred to by the synonyms 1,25(OH)2D3, calcitriol or vitamin D) in blunting the growth of cancer cells is amply recognized. In this review we focused our attention on the cross-talk between 1,25 (OH)2D3 and the tumor...

    journal_title:Anticancer research

    pub_type: 杂志文章,评审

    doi:10.21873/anticanres.11216

    authors: Shany S,Sigal-Batikoff I,Lamprecht S

    更新日期:2016-12-01 00:00:00

  • Anti-tumor effect of in vivo IL-2 and GM-CSF electrogene therapy in murine hepatoma model.

    abstract:BACKGROUND:We evaluated the effect of in vivo electrogene therapy (EGT), a newly-developed gene transfer method using electroporation on the induction of anti-cancer immunity. MATERIALS AND METHODS:The in vivo EGT was carried out by direct injection of plasmid DNAs encoding mouse interleukin-2 (IL-2) and granulocyte-m...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Chi CH,Wang YS,Lai YS,Chi KH

    更新日期:2003-01-01 00:00:00

  • DANCR Acts as a Diagnostic Biomarker and Promotes Tumor Growth and Metastasis in Hepatocellular Carcinoma.

    abstract:BACKGROUND:Long non-coding RNA differentiation antagonizing non-protein coding RNA (DANCR) is considered to be an oncogene in many cancer types. However, the role of DANCR in diagnosis and progression of hepatocellular carcinoma (HCC) is still unknown. PATIENTS AND METHODS:In this study, 146 participants including hea...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.11236

    authors: Ma X,Wang X,Yang C,Wang Z,Han B,Wu L,Zhuang L

    更新日期:2016-12-01 00:00:00

  • LINE-1 Hypomethylation Is Associated With Malignant Traits and Cell Proliferation in Lung Adenocarcinoma.

    abstract:BACKGROUND/AIM:Long interspersed nuclear element-1 (LINE-1) methylation status is a marker for global DNA methylation. However, the relationship between LINE-1 methylation and the biology of lung adenocarcinoma remains unclear. Here, we aimed to examine the role of LINE-1 in lung cancer. MATERIALS AND METHODS:LINE-1 m...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:10.21873/anticanres.14579

    authors: Kitahara H,Okamoto T,Shimamatsu S,Kohno M,Morodomi Y,Tagawa T,Kitao H,Okano S,Oda Y,Maehara Y,Mori M

    更新日期:2020-10-01 00:00:00

  • Vinorelbine and cisplatin in patients with advanced non-small cell lung cancer with interstitial pneumonia.

    abstract:AIM:The aim of the present study was to investigate the efficacy and tolerability of vinorelbine and cisplatin for the treatment of patients with advanced (stage IIIB, IV or relapse) non-small cell lung cancer (NSCLC) with interstitial pneumonia (IP). PATIENTS AND METHODS:A total of 67 patients treated with vinorelbin...

    journal_title:Anticancer research

    pub_type: 杂志文章

    doi:

    authors: Watanabe N,Niho S,Kirita K,Umemura S,Matsumoto S,Yoh K,Ohmatsu H,Goto K

    更新日期:2015-03-01 00:00:00