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DNA-reactive anticancer imidazoacridinone C-1311 is a new inhibitor of hypoxia-inducible factor 1 alpha, vascular endothelial growth factor and tumor angiogenesis
PublikacjaHypoxia-inducible factor 1 (HIF-1) plays a critical role for tumor adaptation to hypoxia and promotes angiogenesis. Antitumor imidazoacridinone C-1311 is a DNA reactive topoisomerase II and FLT3 receptor tyrosine kinase inhibitor selected for phase II clinical trials for breast cancer. Here, we demonstrate the new mechanism of C-1311 action involving HIF-1a, vascular endothelial growth factor (VEGF) and angiogenesis as additional...
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Aberration of the enzymatic activity of Fhit tumor suppressor protein enhances cancer cell death upon photodynamic therapy similarly to that driven by wild-type Fhit
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Analysis of Circulating Tumor Cells in Patients with Non-Metastatic High-Risk Prostate Cancer before and after Radiotherapy Using Three Different Enumeration Assays
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Impedimetric Detection of Femtomolar Levels of Interleukin 6, Interleukin 8, and Tumor Necrosis Factor Alpha Based on Thermally Modified Nanotubular Titanium Dioxide Arrays
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Cancer stem cells and escape from drug-induced premature senescence in human lung tumor cells: implications for drug resistance and in vitro drug screening models
PublikacjaBadania z użyciem modelu komórek nowotworu płuc A549 wykazały, że komórki te po traktowaniu lekami uszkadzającymi DNA zatrzymują proliferację i wchodzą w stan starzenia komórkowego. Jednak post-inkubacja tych komórek prowadzi do powrotu do stanu proliferacji małej frakcji komórek. Wykazaliśy, że frakcja ta związana jest z obecnością komórek pierwotnych nowotworu w populacji komórek A549. Powrót do stanu proliferacji komóek A549...
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Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia
PublikacjaInduction of proteins involved in drug metabolism and in drug delivery has a significant impact on drug-drug interactions and on the final therapeutic effects. Two antitumor acridine derivatives selected for present studies, C-1748 (9-(2’-hydroxyethylamino)-4-methyl-1-nitroacridine) and C-1305 (5-dimethylaminopropylamino-8-hydroxy-triazoloacridinone), expressed high and low susceptibility to metabolic transformations with liver...
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Pronounced cytostatic activity and bystander effect of a novel series of fluorescent tricyclic acyclovir and ganciclovir derivatives in herpes simplex virus thymidine kinase gene-transduced tumor cell lines
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The activity of latent benzoperimidine esters to inhibit P-glycoprotein and multidrug resistance-associated protein 1 dependent efflux of pirarubicin from several lines of multidrug resistant tumor cells.
PublikacjaZaprezentowano wyniki badań biologicznych przeprowadzonych dla nowej grupy związków: estrów benzoperymidyny z zastosowaniem wybranych linii komórek nowotworowych: wrażliwych i opornych o oporności P-gp-zależnej, MRP1-zależnej i o oporności związanej z nadekspresją białek MRP1/LRP. Metodą spektrofluorymetryczną zbadano zdolność estrów benzoperymidyny do hamowania eksportu aktywnego pirarubicyny z komórek opornych. Estry benzoperymidyny...
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublikacjaIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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Effect of modification of 6-[(aminoalkyl)amino]-7H-benzo[e]-perimidin-7-ones on their cytotoxic activity toward sensitive and multidrug resistant tumor cell lines. Synthesis and biological evaluation
PublikacjaPrzeprowadzono syntezę szeregu nowych pochodnych benzoperimidynowych, a mianowicie: monohydroksybenzoperimidyny i 2-aminobenzoperimidyny. Oznaczono aktywność przeciwnowotworową in vitro powyższych związków względem komórek nowotworowych bez oporności oraz z wykształconą opornością wielolekową. Wyznaczono również powinowactwo pochodnych do błony komórkowej, na kolumnie HPLC z odpowiednim wypełnieniem.
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Expression of selected epithelial–mesenchymal transition transcription factors in serous borderline ovarian tumors and type I ovarian cancers
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KRAS mutation testing in borderline ovarian tumors and low-grade ovarian carcinomas with a rapid, fully integrated molecular diagnostic system
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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublikacjaA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublikacjaA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Prognostic significance of pretreatment VEGF, survivin, and Smac/DIABLO serum levels in patients with serous ovarian carcinoma
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The methylation of a panel of genes differentiates low-grade from high-grade gliomas
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Determination of BRAF V600E (VE1) protein expression and BRAF gene mutation status in codon 600 in borderline and low-grade ovarian cancers
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Antitumor Activity of Triazine Mimic Antibiotics for DNA-binding Implications (Impressive Activity in Vitro Against a Variety of Tumor Types in the NCI-60 Screen): NSC 710607 To Fight HCT-116 Human Colon Carcinoma Cell Lines in Vivo Using the Hollow Fiber Assay and Xenograft Mouse Models
PublikacjaPurpose Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. Methods The NCI initial hollow...
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Reduced expression of ELAVL4 in male meningioma patients
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Automatische Tumorsegmentierung mit spärlich annotierter Lernbasis
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Überwachtes Lernen zur Prädiktion von Tumorwachstum
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Simplifying biochemical tumorous bone remodeling models through variable order derivatives
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The Anti-Tumoral Potential of Phosphonate Analog of Sulforaphane in Zebrafish Xenograft Model
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Evaluation of survivin splice variants in pituitary tumors
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Role of Src Kinases in Neu-Induced Tumorigenesis: Challenging the Paradigm Using Csk Homologous Kinase Transgenic Mice
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Metastasis of the testicular germ cell tumors to the parotid gland
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Diagnosis of Brain Tumors Through Global Specific DNA Methylation Analysis
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Baseline chromogranin A and its dynamics are prognostic markers in gastroenteropancreatic neuroendocrine tumors
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Bariatric surgery and incidental gastrointestinal stromal tumors – a single-center study
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Chemometric Evaluation of Urinary Steroid Hormone Levels as Potential Biomarkers of Neuroendocrine Tumors
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Molecular Characterization of Growth Hormone-producing Tumors in the GC Rat Model of Acromegaly
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Rapid PD-L1 detection in tumors with PET using a highly specific peptide
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Regarding the “Review of surgical techniques and guide for decision making in the treatment of benign parotid tumors”
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Germ cell-like telomeric length homeostasis in nonseminomatous testicular germ cell tumors
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Microneedle‐Based Generation of Microbubbles in Cancer Tumors to Improve Ultrasound‐Assisted Drug Delivery
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Classification of Thyroid Tumors Based on Mass Spectrometry Imaging of Tissue Microarrays; a Single-Pixel Approach
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Testing for NRAS Mutations in Serous Borderline Ovarian Tumors and Low-Grade Serous Ovarian Carcinomas
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<p>Nanomechanics and Histopathology as Diagnostic Tools to Characterize Freshly Removed Human Brain Tumors</p>
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Positive electrostatic therapy of metastatic tumors: selective induction of apoptosis in cancer cells by pure charges
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What are the true volumes of SEGA tumors? Reliability of planimetric and popular semi-automated image segmentation methods
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Radiochemical Synthesis and Evaluation of Novel Radioconjugates of Neurokinin 1 Receptor Antagonist Aprepitant Dedicated for NK1R-Positive Tumors
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A targeted mass spectrometry immunoassay to quantify osteopontin in fresh-frozen breast tumors and adjacent normal breast tissues
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Coincidental Detection of Gastrointestinal Stromal Tumors During Laparoscopic Bariatric Procedures—Data and Treatment Strategy of a German Reference Center
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Expression of zinc finger transcription factors (ZNF143 and ZNF281) in serous borderline ovarian tumors and low-grade ovarian cancers
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Molecular Heterogeneity of Papillary Thyroid Cancer: Comparison of Primary Tumors and Synchronous Metastases in Regional Lymph Nodes by Mass Spectrometry Imaging
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The associations between serum VEGF, bFGF and endoglin levels with microvessel density and expression of proangiogenic factors in malignant and benign ovarian tumors
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Expression-based decision tree model reveals distinct microRNA expression pattern in pediatric neuronal and mixed neuronal-glial tumors
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LanroNET, a non-interventional, prospective study to assess the resource utilization and cost of lanreotide autogel 120 mg in Polish patients with neuroendocrine tumors – results of interim analysis
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Corrigendum to “Rapid PD-L1 detection in tumors with PET using a highly specific peptide” [Biochemical and Biophysical Research Communications 483/1 (2017) 258–263]
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublikacjaNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...