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https://www.readbyqxmd.com/read/28304114/antiviral-and-cytostatic-evaluation-of-5-1-halo-2-sulfonylvinyl-and-5-2-furyl-uracil-nucleosides
#1
Zhiwei Wen, Sazzad H Suzol, Jufang Peng, Yong Liang, Robert Snoeck, Graciela Andrei, Sandra Liekens, Stanislaw F Wnuk
Transition metal-catalyzed halosulfonylation of 5-ethynyl uracil nucleosides provided (E)-5-(1-chloro-2-tosylvinyl)uridines. Tetrabutylammonium fluoride-mediated direct CH arylation of 5-iodouracil nucleosides with furan or 2-heptylfuran gave 5-furyl-substituted nucleosides without the necessity of using the organometallic substrates. These two classes of 5-substituted uracil nucleosides as well their corresponding ester derivatives were tested against a broad range of DNA and RNA viruses and the human immunodeficiency virus (HIV)...
March 17, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28290674/copper-i-phosphine-polypyridyl-complexes-synthesis-characterization-dna-hsa-binding-study-and-antiproliferative-activity
#2
Wilmer Villarreal, Legna Colina-Vegas, Gonzalo Visbal, Oscar Corona, Rodrigo S Corrêa, Javier Ellena, Marcia Regina Cominetti, Alzir Azevedo Batista, Maribel Navarro
A series of copper(I)-phosphine polypyridyl complexes have been investigated as potential antitumor agents. The complexes [Cu(PPh3)2dpq]NO3 (2), [Cu(PPh3)2dppz]NO3 (3), [Cu(PPh3)2dppa]NO3 (4), and [Cu(PPh3)2dppme]NO3 (5) were synthesized by the reaction of [Cu(PPh3)2NO3] with the respective planar ligand under mild conditions. These copper complexes were fully characterized by elemental analysis, molar conductivity, FAB-MS, and NMR, UV-vis, and IR spectroscopies. Interactions between these copper(I)-phosphine polypyridyl complexes and DNA have been investigated using various spectroscopic techniques and analytical methods, such as UV-vis titrations, thermal denaturation, circular dichroism, viscosity measurements, gel electrophoresis, and competitive fluorescent intercalator displacement assays...
March 14, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28274414/evaluation-of-the-characteristics-of-some-plant-polyphenols-as-molecules-intercepting-mitoxantrone
#3
Adam Osowski, Adam Kasparek, Zbigniew Wieczorek, Ryszard Amarowicz, Mariusz Szabelski
This paper contains the results of a study on the interactions between mitoxantrone and some bioactive polyphenols. It has been demonstrated that polyphenols can intercept mitoxantrone. Quercetin shows the highest affinity for complexing with mitoxantrone, in contrast to resveratrol, which shows the lowest affinity. The main process underlying the association between cytostatic and polyphenols occurs in the ground state. The values of the constants of the association reactions between the analysed compounds and mitoxantrone are large enough to generate an evident intercepting effect in the three-component system (mitoxantrone-DNA-polyphenol)...
July 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28272795/inhibition-of-prostate-cancer-proliferation-by-deferiprone
#4
Rui V Simões, Suresh Veeraperumal, Inna S Serganova, Natalia Kruchevsky, Joseph Varshavsky, Ronald G Blasberg, Ellen Ackerstaff, Jason A Koutcher
Cancer growth and proliferation rely on intracellular iron availability. We studied the effects of Deferiprone (DFP), a chelator of intracellular iron, on three prostate cancer cell lines: murine, metastatic TRAMP-C2; murine, non-metastatic Myc-CaP; and human, non-metastatic 22rv1. The effects of DFP were evaluated at different cellular levels: cell culture proliferation and migration; metabolism of live cells (time-course multi-nuclear magnetic resonance spectroscopy cell perfusion studies, with 1-(13) C-glucose, and extracellular flux analysis); and expression (Western blot) and activity of mitochondrial aconitase, an iron-dependent enzyme...
March 8, 2017: NMR in Biomedicine
https://www.readbyqxmd.com/read/28266296/complete-tubal-abortion-a-rare-form-of-ectopic-pregnancy
#5
Bogdan Chirculescu, Raluca Chirculescu, Mioara Ionescu, Gheorghe Peltecu, Anca Panaitescu
Tubal abortion is characterized by the extrusion of an ectopic product of conception implanted in the fallopian tube through the abdominal ostium into the peritoneal cavity. It can be either complete or incomplete and may lead to severe bleeding. Recognition of a complete tubal abortion may be challenging but is essential because it allows conservative management which make possible preservation of tubal function and fertility without the need for further cytostatic therapy. A case of a 30 years-old woman admitted for lower abdominal pain is reported...
January 2017: Chirurgia
https://www.readbyqxmd.com/read/28266278/synthesis-and-preliminary-cytotoxicity-studies-of-1-1-4-5-dihydrooxazol-2-yl-1h-indazol-3-yl-3-phenylurea-and-3-phenylthiourea-derivatives
#6
Monika Wojciechowska, Łukasz Sitek, Aneta Sakowicz, Ewa Romejko, Piotr Szumlas, Martyna Korcz, Patrick J Bednarski, Franciszek Sączewski, Anita Kornicka
BACKGROUND: N-substituted 3-amino-1H-indazoles represent an interesting class of biologically active compounds. Among them, derivatives containing phenylurea moiety are of particular interest. Such compounds have been found to possess inhibitory activity against cancer cell growth. Additionally, various oxazoline-containing compounds have also been designed as potential anticancer agents. OBJECTIVE: The aim of this work was to obtain a new class of N-substituted 3-amino-1H-indazole derivatives with cytotoxic activity towards cancer cells...
March 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28263527/genotoxicity-of-wastewater-from-health-care-facilities
#7
Alena Vlková, Zdeňka Wittlingerová, Magdalena Zimová, Gabriela Jírová, Kristina Kejlová, Stanislav Janoušek, Dagmar Jírová
Health care facilities use for therapeutic purposes, diagnostics, research, and disinfection a high number of chemical compounds, such as pharmaceuticals (e.g. antibiotics, cytostatics, antidepressants), disinfectants, surfactants, metals, radioactive elements, bleach preparations, etc. Hospitals consume significant amounts of water (in the range of 400 to 1200 liters/day/bed) corresponding to the amount of wastewater discharge. Some of these chemicals are not eliminated in wastewater treatment plants and are the source of pollution for surface and groundwater supplies...
December 18, 2016: Neuro Endocrinology Letters
https://www.readbyqxmd.com/read/28260860/antiproliferation-effect-of-imatinib-mesylate-on-mcf7-t-47d-tumorigenic-and-mcf-10a-nontumorigenic-breast-cell-lines-via-pdgfr-%C3%AE-pdgf-bb-c-kit-and-scf-genes
#8
Ali Kadivar, Behnam Kamalidehghan, Hamid Akbari Javar, Benyamin Karimi, Reihaneh Sedghi, Mohamed Ibrahim Noordin
Recent cancer molecular therapies are targeting main functional molecules to control applicable process of cancer cells. Attractive targets are established by receptor tyrosine kinases, such as platelet-derived growth factor receptors (PDGFRs) and c-Kit as mostly irregular signaling, which is due to either over expression or mutation that is associated with tumorigenesis and cell proliferation. Imatinib mesylate is a selective inhibitor of receptor tyrosine kinase, including PDGFR-β and c-Kit. In this research, we studied how imatinib mesylate would exert effect on MCF7 and T-47D breast cancer and MCF 10A epithelial cell lines, the gene and protein expression of PDGFR-β, c-Kit and their relevant ligands platelet-derived growth factor (PDGF)-BB and stem cell factor (SCF)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28259616/observational-retrospective-study-of-vascular-modulator-changes-during-treatment-in-essential-thrombocythemia
#9
Andrea Piccin, Michael Steurer, Clemens Feistritzer, Ciaran Murphy, Elva Eakins, Muriel Van Schilfgaarde, Daisy Corvetta, Angela Maria Di Pierro, Irene Pusceddu, Luigi Marcheselli, Roberto Gambato, Martin Langes, Dino Veneri, Omar Perbellini, Enrica Pacquola, Michele Gottardi, Filippo Gherlinzoni, Andrea Mega, Martina Tauber, Guido Mazzoleni, Elisa Piva, Mario Plebani, Mauro Krampera, Günther Gastl
Essential thrombocythemia (ET) patients are at risk of developing thrombotic events. Qualitative platelet (PLT) abnormalities and activation of endothelial cells (ECs) and PLTs are thought to be involved. Microparticles (MPs) can originate from PLTs (PMPs), ECs (EMPs), or red cells (RMPs). Previous studies have indicated that MPs contribute to ET pathophysiology. Endothelial modulators (eg, nitric oxide [NO], adrenomedullin [ADM], and endothelin-1 [ET-1]) are also involved in the pathophysiology of this condition...
February 14, 2017: Translational Research: the Journal of Laboratory and Clinical Medicine
https://www.readbyqxmd.com/read/28258797/synthesis-and-evaluation-of-5-arylthio-9h-pyrimido-4-5-b-indole-2-4-diamines-as-receptor-tyrosine-kinase-and-thymidylate-synthase-inhibitors-and-as-antitumor-agents
#10
Nilesh Zaware, Roy Kisliuk, Anja Bastian, Michael A Ihnat, Aleem Gangjee
In an effort to optimize the structural requirements for combined cytostatic and cytotoxic effects in single agents, a series of 5-(arylthio)-9H-pyrimido[4,5-b]indole-2,4-diamines 3-7 were synthesized and evaluated as inhibitors of receptor tyrosine kinases (RTKs) as well as thymidylate synthase (TS). The synthesis of these compounds involved the nucleophilic displacement of the common intermediate 5-bromo/5-chloro-9H-pyrimido[4,5-b]indole-2,4-diamine with appropriate aryl thiols. A novel four step synthetic scheme to the common intermediate was developed which is more efficient relative to the previously reported six-step sequence...
April 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28258670/the-role-of-metallothionein-in-oncogenesis-and-cancer-treatment
#11
Anna Bizoń, Kinga Jędryczko, Halina Milnerowicz
Metallothionein is cysteine-rich low molecular mass protein. The involvement of MT in many physiological and pathophysiological processes such as apoptosis, proliferation, angiogenesis, and the detoxification of heavy metals suggested participation of this protein in carcinogenesis and tumor therapy. Depending on the type of tissue and classification of carcinoma various it was observed relation between MT expression and tumor type, stage, grade, poor prognosis and body resistance to radiotherapy and chemotherapy...
February 14, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28257497/investigating-antimalarial-drug-interactions-of-emetine-dihydrochloride-hydrate-using-calcusyn-based-interactivity-calculations
#12
Holly Matthews, Jon Deakin, May Rajab, Maryam Idris-Usman, Niroshini J Nirmalan
The widespread introduction of artemisinin-based combination therapy has contributed to recent reductions in malaria mortality. Combination therapies have a range of advantages, including synergism, toxicity reduction, and delaying the onset of resistance acquisition. Unfortunately, antimalarial combination therapy is limited by the depleting repertoire of effective drugs with distinct target pathways. To fast-track antimalarial drug discovery, we have previously employed drug-repositioning to identify the anti-amoebic drug, emetine dihydrochloride hydrate, as a potential candidate for repositioned use against malaria...
2017: PloS One
https://www.readbyqxmd.com/read/28252422/sorption-correction-of-nephron-sub-microscopic-changes-caused-by-neoplastic-chronic-intoxication-with-the-application-of-cytostatic-therapy
#13
Yu Soroka, N Lisnychuk, I Demkiv, O Oleshchuk
The electron microscopic changes of the nephron structural components under conditions of dimethylhydrazine (DMH)-induced carcinogenesis with the development of colorectal adenocarcinoma in situ were evaluated. Destructive changes in epitheliocytes of proximal and distal tubules of the nephron, microcirculation disturbances in renal corpuscles and tubular structure are evidences of disorder in urine formation stages. Аdministration of cytostatics aggravates the degree of destructive changes in the kidney. The application of carbon enterosorbent of IV generation "Carboline" for chronic neoplastic endotoxemia correction in combination with chemotherapy components significantly reduces the structural changes of the cortical substance of the kidneys, activates processes of reparative regeneration...
January 2017: Georgian Medical News
https://www.readbyqxmd.com/read/28249907/hdac-inhibitor-panobinostat-engages-host-innate-immune-defenses-to-promote-the-tumoricidal-effects-of-trastuzumab-in-her2-tumors
#14
Mikolaj Medon, Eva Vidacs, Stephin J Vervoort, Jason Li, Misty R Jenkins, Kelly M Ramsbottom, Joseph A Trapani, Mark J Smyth, Phillip K Darcy, Peter W Atadja, Michael A Henderson, Ricky W Johnstone, Nicole M Haynes
Histone deacetylase inhibitors (HDACi) may engage host immunity as one basis for their antitumor effects. Herein we demonstrate an application of this concept using the HDACi panobinostat to augment the antitumor efficacy of trastuzumab (anti-HER2) therapy, through both tumor cell autonomous and non-autonomous mechanisms. In HER2+ tumors that are inherently sensitive to the cytostatic effects of trastuzumab, co-treatment with panobinostat abrogated AKT signaling and triggered tumor regression in mice that lacked innate and/or adaptive immune effector cells...
March 1, 2017: Cancer Research
https://www.readbyqxmd.com/read/28246180/tgf-%C3%AE-family-signaling-in-tumor-suppression-and-cancer-progression
#15
Joan Seoane, Roger R Gomis
Transforming growth factor-β (TGF-β) induces a pleiotropic pathway that is modulated by the cellular context and its integration with other signaling pathways. In cancer, the pleiotropic reaction to TGF-β leads to a diverse and varied set of gene responses that range from cytostatic and apoptotic tumor-suppressive ones in early stage tumors, to proliferative, invasive, angiogenic, and oncogenic ones in advanced cancer. Here, we review the knowledge accumulated about the molecular mechanisms involved in the dual response to TGF-β in cancer, and how tumor cells evolve to evade the tumor-suppressive responses of this signaling pathway and then hijack the signal, converting it into an oncogenic factor...
February 28, 2017: Cold Spring Harbor Perspectives in Biology
https://www.readbyqxmd.com/read/28230826/modifying-effects-of-5-azacytidine-on-metal-containing-proteins-profile-in-guerin-carcinoma-with-different-sensitivity-to-cytostatics
#16
V F Chekhun, Y V Lozovska, L A Naleskina, T V Borikun, A P Burlaka, I N Todor, D V Demash, T M Yalovenko, T V Zadvornyi, A O Pavlova, D M Storchay, N Yu Lukianova
AIM: To assess the influence of the treatment with 5-azacytidine (5-aza) on the profile of metal-containing proteins and factors of their regulation in Guerin carcinoma cells in vivo. MATERIALS AND METHODS: The study was conducted on Wistar rats transplanted with wild-type Guerin carcinoma (Guerin/WT) and its strains resistant to cisplatin (Guerin/CP) or doxorubicin (Guerin/Dox). Animals were distributed in 6 groups treated with 5-aza and control animals without treatment...
December 2016: Experimental Oncology
https://www.readbyqxmd.com/read/28222315/allylic-isothiouronium-salts-the-discovery-of-a-novel-class-of-thiourea-analogues-with-antitumor-activity
#17
Misael Ferreira, Laura Sartori Assunção, Adny Henrique Silva, Fabíola Branco Filippin-Monteiro, Tânia Beatriz Creczynski-Pasa, Marcus Mandolesi Sá
A series of 28 aryl- and alkyl-substituted isothiouronium salts were readily synthesized in high yields through the reaction of allylic bromides with thiourea, N-monosubstituted thioureas or thiosemicarbazide. The S-allylic isothiouronium salts substituted with aliphatic groups were found to be the most effective against leukemia cells. These compounds combine high antitumor activity and low toxicity toward non-tumoral cells, with selectivity index higher than 20 in some cases. Furthermore, the selected isothiouronium salts induced G2/M cell cycle arrest and cell death, possibly by apoptosis...
March 31, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28221790/synthesis-and-cytostatic-and-antiviral-profiling-of-thieno-fused-7-deazapurine-ribonucleosides
#18
Michal Tichý, Sabina Smoleń, Eva Tloušt'ová, Radek Pohl, Tomáš Oždian, Klára Hejtmánková, Barbora Lišková, Soňa Gurská, Petr Džubák, Marián Hajdúch, Michal Hocek
Two isomeric series of new thieno-fused 7-deazapurine ribonucleosides (derived from 4-substituted thieno[2',3':4,5]pyrrolo[2,3-d]pyrimidines and thieno[3',2':4,5]pyrrolo[2,3-d]pyrimidines) were synthesized by a sequence involving Negishi coupling of 4,6-dichloropyrimidine with iodothiophenes, nucleophilic azidation, and cyclization of tetrazolopyrimidines, followed by glycosylation and cross-couplings or nucleophilic substitutions at position 4. Most nucleosides (from both isomeric series) exerted low micromolar or submicromolar in vitro cytostatic activities against a broad panel of cancer and leukemia cell lines and some antiviral activity against HCV...
March 3, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28218725/treating-cancer-by-targeting-telomeres-and-telomerase
#19
REVIEW
Marko Ivancich, Zachary Schrank, Luke Wojdyla, Brandon Leviskas, Adijan Kuckovic, Ankita Sanjali, Neelu Puri
Telomerase is expressed in more than 85% of cancer cells. Tumor cells with metastatic potential may have a high telomerase activity, allowing cells to escape from the inhibition of cell proliferation due to shortened telomeres. Human telomerase primarily consists of two main components: hTERT, a catalytic subunit, and hTR, an RNA template whose sequence is complimentary to the telomeric 5'-dTTAGGG-3' repeat. In humans, telomerase activity is typically restricted to renewing tissues, such as germ cells and stem cells, and is generally absent in normal cells...
February 19, 2017: Antioxidants (Basel, Switzerland)
https://www.readbyqxmd.com/read/28218046/thyroid-transcription-factor-1-expression-is-associated-with-outcome-of-patients-with-non-squamous-non-small-cell-lung-cancer-treated-with-pemetrexed-based-chemotherapy
#20
Ondrej Fiala, Milos Pesek, Jana Skrickova, Vitezslav Kolek, Frantisek Salajka, Marcela Tomiskova, Monika Satankova, Juraj Kultan, Jana Kuliskova, Martin Svaton, Michal Hrnciarik, Karel Hejduk, Renata Chloupkova, Ondrej Topolcan, Helena Hornychova, Marketa Nova, Ales Ryska, Jindrich Finek
Pemetrexed is an antifolate cytostatic agent targeting several folate-dependent enzymatic pathways, widely used in the treatment of locally advanced or metastatic stage non-small cell lung cancer. Aside from the non-squamous histology, there is still no available molecular biomarker predicting treatment efficacy of pemetrexed-based chemotherapy. The aim of our retrospective study was to evaluate the association of thyroid transcription factor 1 expression with outcome of a large cohort of patients with non-squamous non-small cell lung cancer treated with pemetrexed...
February 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
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