Synthesis, anti-HIV-1 and antiproliferative evaluation of novel 4-nitroimidazole derivatives combined with 5-hydroxy-4-pyridinone moiety

Publication date: 15 February 2020Source: Journal of Molecular Structure, Volume 1202Author(s): Pouria Shirvani, Afshin Fassihi, Lotfollah Saghaie, Siska Van Belle, Zeger Debyser, Frauke ChristAbstractIn an effort to synthesize more effective non-nucleoside reverse transcriptase inhibitors (NNRTIs) against the HIV-1 infection, a new series of novel 4-nitroimidazole derivatives combined with 5-hydroxy-4-pyridinone moiety were designed by molecular docking studies, prepared and characterized by spectroscopic techniques. All the synthesized compounds were in vitro evaluated for their inhibitory effect against the HIV-1 replication in the MT-4 cells. Results showed that none of these synthesized compounds displayed any specific anti HIV-1 activity. Surprisingly, these compounds showed high cytotoxicity against MT-4 cells with low selectivity index (
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research

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Publication date: Available online 22 January 2020Source: Mutation Research/Genetic Toxicology and Environmental MutagenesisAuthor(s): Donna Goodenow, Faith Emmanuel, Chase Berman, Mark Sahyouni, Christine RichardsonAbstractBioflavonoids have a similar chemical structure to etoposide, the well-characterized topoisomerase II (Top2) poison, and evidence shows that they also induce DNA double-strand breaks (DSBs) and promote genome rearrangements. The purpose of this study was to determine the kinetics of bioflavonoid-induced DSB appearance and repair, and their dependence on Top2. Cells were exposed to bioflavonoids individu...
Source: Mutation Research Genetic Toxicology and Environmental Mutagenesis - Category: Genetics & Stem Cells Source Type: research
This study closed early due to accrual and is registered with the UMIN Clinical Trials Registry (UMIN000011099).FindingsBetween Sept 20, 2013 and July 12, 2016, 68 patients who had a deep molecular response after receiving first-line dasatinib for at least 24 months were enrolled and assigned to the consolidation phase. Nine patients were excluded during the consolidation phase and one patient was excluded after study completion because of meeting exclusion criteria. 58 patients discontinued dasatinib and were assessed. 32 (55%) of 58 patients had treatment-free remission at 6 months after dasatinib discontinuation, and me...
Source: The Lancet Haematology - Category: Hematology Source Type: research
Publication date: Available online 21 January 2020Source: The Lancet HaematologyAuthor(s): Massimo Breccia, Robin Foà
Source: The Lancet Haematology - Category: Hematology Source Type: research
Conditions:   Haematological Malignancy;   Leukemia, Acute;   Lymphoma;   Myeloma Multiple;   Blood Cancer;   Quality of Life Intervention:   Other: WHODAS 2.0 Questionnaire Sponsor:   University of Malaya Recruiting
Source: - Category: Research Source Type: clinical trials
ConclusionTh17 cells contribute to the stratification of different treatment stages of MM patients. The level of Th17 cells in patients with newly diagnosed MM is associated with the treatment outcome of complete remission.
Source: Clinical Lymphoma Myeloma and Leukemia - Category: Cancer & Oncology Source Type: research
Publication date: 21 January 2020Source: Cell Reports, Volume 30, Issue 3Author(s): Etienne Paubelle, Florence Zylbersztejn, Thiago Trovati Maciel, Caroline Carvalho, Annalisa Mupo, Meyling Cheok, Liesbet Lieben, Pierre Sujobert, Justine Decroocq, Akihiko Yokoyama, Vahid Asnafi, Elizabeth Macintyre, Jérôme Tamburini, Valérie Bardet, Sylvie Castaigne, Claude Preudhomme, Hervé Dombret, Geert Carmeliet, Didier Bouscary, Yelena Z. GinzburgSummaryVitamin D (VD) is a known differentiating agent, but the role of VD receptor (VDR) is still incompletely described in acute myeloid leukemia (AML), whose tre...
Source: Cell Reports - Category: Cytology Source Type: research
Authors: Wu J, Li YT, Tian XT, Liu YS, Wu ML, Li PN, Liu J Abstract BACKGROUNDS: Anaplastic thyroid cancer/ATC is highly lethal malignancy without reliable chemotherapeutic drug. Resveratrol possesses anti-ATC activities but encounters resistance in some cases due to certain unknown reason(s). OBJECTIVE: Because signal transducer and activator of transcription/STAT3 signaling is critical for ATC cell survival and the main molecular target of resveratrol, its roles in determining the fates of resveratrol-treated ATC cells were investigated here. METHODS: Human THJ-11T, THJ-16 and THJ-21T ATC cell lines were ...
Source: Cancer Biomarkers - Category: Cancer & Oncology Tags: Cancer Biomark Source Type: research
In conclusion, miR- 1290 promoted proliferation and suppressed apoptosis in AML by targeting FOXG1 and SOCS3, which might provide a therapeutic target for AML. PMID: 31960662 [PubMed - in process]
Source: Journal of Biological Regulators and Homeostatic Agents - Category: Biomedical Science Tags: J Biol Regul Homeost Agents Source Type: research
Kathryn Cartwright, of Sutton, Coldfield, became an inspirational figure since her leukaemia diagnosis 13 years ago. She died of an 'insurmountable' liver infection on January 18.
Source: the Mail online | Health - Category: Consumer Health News Source Type: news
The protein-protein interaction between menin and mixed lineage leukemia 1 (MLL1) plays a critical role in acute leukemias with translocations of the MLL1 gene or with mutations in the nucleophosmin 1 (NPM1) gene. As a step toward clinical translation of menin-MLL1 inhibitors, we report development of MI-3454, a highly potent and orally bioavailable inhibitor of the menin-MLL1 interaction. MI-3454 profoundly inhibited proliferation and induced differentiation in acute leukemia cells and primary patient samples with MLL1 translocations or NPM1 mutations. When applied as a single agent, MI-3454 induced complete remission or ...
Source: Journal of Clinical Investigation - Category: Biomedical Science Authors: Source Type: research
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