keyword
MENU ▼
Read by QxMD icon Read
search

Compound a

keyword
https://www.readbyqxmd.com/read/28351128/nanoparticles-of-titanium-and-zinc-oxides-as-novel-agents-in-tumor-treatment-a-review
#1
Janusz Bogdan, Joanna Pławińska-Czarnak, Joanna Zarzyńska
Cancer has become a global problem. On all continents, a great number of people are diagnosed with this disease. In spite of the progress in medical care, cancer still ends fatal for a great number of the ill, either as a result of a late diagnosis or due to inefficiency of therapies. The majority of the tumors are resistant to drugs. Thus, the search for new, more effective therapy methods continues. Recently, nanotechnology has been attributed with big expectations in respect of the cancer fight. That interdisciplinary field of science creates nanomaterials (NMs) and nanoparticles (NPs) that can be applied, e...
December 2017: Nanoscale Research Letters
https://www.readbyqxmd.com/read/28351064/the-early-tech-development-course-experiential-commercialization-education-for-the-medical-academician
#2
Jonathan Servoss, Connie Chang, Jonathan Fay, Kevin Ward
PROBLEM: Research produced by medical academicians holds promise for developing into biomedical innovations in therapeutics, devices, diagnostics, and health care information technology; however, the road to biomedical innovation is fraught with risk, including the challenge of moving from basic research insight onto a viable commercialization path. Compounding this challenge is the growing demand on medical academicians to be more productive in their clinical, teaching, and research duties within a resource-constrained environment...
April 2017: Academic Medicine: Journal of the Association of American Medical Colleges
https://www.readbyqxmd.com/read/28351032/baicalein-a-natural-anti-cancer-compound-alters-microrna-expression-profiles-in-bel-7402-human-hepatocellular-carcinoma-cells
#3
Beibei Bie, Jin Sun, Jun Li, Ying Guo, Wei Jiang, Chen Huang, Jun Yang, Zongfang Li
BACKGROUND/AIMS: Baicalein has been shown to possess significant anti-hepatoma activity by inhibiting cell proliferation. Whether the anti-proliferative effect of baicalein is related to its modulation of miRNA expression in hepatocellular carcinoma (HCC) is still unknown. METHODS: The anti-proliferative effects of baicalein on HCC cell line Bel-7402 was assessed by detecting the proliferation activity, cell cycle distribution, expression changes of p21/CDKN1A, P27/CDKN1B, total Akt and phosphoryted AKT...
March 24, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28351017/performance-of-a-docking-molecular-dynamics-protocol-for-virtual-screening-of-nutlin-class-inhibitors-of-mdmx
#4
Nagakumar Bharatham, Kristin E Finch, Jaeki Min, Anand Mayasundari, Michael A Dyer, R Kiplin Guy, Donald Bashford
A virtual screening protocol involving docking and molecular dynamics has been tested against the results of fluorescence polarization assays testing the potency of a series of compounds of the nutlin class for inhibition of the interaction between p53 and Mdmx, an interaction identified as a driver of certain cancers. The protocol uses a standard docking method (AutoDock) with a cutoff based on the AutoDock score (ADscore), followed by molecular dynamics simulation with a cutoff based on root-mean-square-deviation (RMSD) from the docked pose...
February 24, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28350999/discovery-of-novel-1-2-3-4-tetrahydrobenzo-4-5-thieno-2-3-c-pyridine-derivatives-as-potent-and-selective-cyp17-inhibitors
#5
Mingliang Wang, Yanjia Fang, Shoulai Gu, Fangfang Chen, Zhengjiang Zhu, Xun Sun, Jidong Zhu
The inhibition of CYP17 to block androgen biosynthesis is a well validated strategy for the treatment of prostate cancer. Herein we reported the design, synthesis and structure-activity relationship (SAR) study for a series of novel 1,2,3,4- tetrahydrobenzo[4,5]thieno[2,3-c]pyridine derivatives. Some analogs demonstrated a potent inhibition to both rat and human CYP17 protein and reduced testosterone production in human H295R cell line. Some analogs also showed high selectivity against other CYP enzymes such as 3A4, 1A2, 2C9, 2C19 and 2D6, which may limit side effects due to drug-drug interactions...
March 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28350997/synthesis-and-biological-evaluation-of-hypoxia-activated-prodrugs-of-sn-38
#6
Chen Jin, Qiumeng Zhang, Wei Lu
We designed new hypoxia-activated prodrugs by conjugating (1-methyl-2-nitro-1H-imidazol-5-yl)methanol with 7-ethyl-10-hydroxy camptothecin (SN-38). Initially, we improved the method of multi-gram scale synthesis of (1-methyl-2-nitro-1H-imidazol-5-yl)methanol, which increased the yield to 42% compared to 8% by the original synthesis method. The improved method was used to synthesize evofosfamide (TH-302) and hypoxia-activated prodrugs of SN-38. Two different linkages between (1-methyl-2-nitro-1H-imidazol-5-yl)methanol and SN-38 were evaluated that afforded different hypoxia-selectivity and toxicity...
March 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28350990/the-putative-drp1-inhibitor-mdivi-1-is-a-reversible-mitochondrial-complex-i-inhibitor-that-modulates-reactive-oxygen-species
#7
Evan A Bordt, Pascaline Clerc, Brian A Roelofs, Andrew J Saladino, László Tretter, Vera Adam-Vizi, Edward Cherok, Ahmed Khalil, Nagendra Yadava, Shealinna X Ge, T Chase Francis, Nolan W Kennedy, Lora K Picton, Tanya Kumar, Sruti Uppuluri, Alexandrea M Miller, Kie Itoh, Mariusz Karbowski, Hiromi Sesaki, R Blake Hill, Brian M Polster
Mitochondrial fission mediated by the GTPase dynamin-related protein 1 (Drp1) is an attractive drug target in numerous maladies that range from heart disease to neurodegenerative disorders. The compound mdivi-1 is widely reported to inhibit Drp1-dependent fission, elongate mitochondria, and mitigate brain injury. Here, we show that mdivi-1 reversibly inhibits mitochondrial complex I-dependent O2 consumption and reverse electron transfer-mediated reactive oxygen species (ROS) production at concentrations (e...
March 27, 2017: Developmental Cell
https://www.readbyqxmd.com/read/28350959/mapping-of-drug-like-chemical-universe-with-reduced-complexity-molecular-frameworks
#8
Aleksejs Kontijevskis
The emergence of DNA-encoded chemical libraries (DEL) field in past decade has attracted attention of pharmaceutical industry as a powerful mechanism for the discovery of novel drug-like hits for various biological targets. Nuevolution Chemetics technology enables DNA encoded synthesis of billions of chemically diverse drug-like small molecule compounds, and the efficient screening and optimization of these, facilitating effective identification of drug candidates at an unprecedented speed and scale. Although many approaches have been developed by the cheminformatics community for the analysis and visualization of drug-like chemical space, most of them are restricted to the analysis of maximum few millions of compounds and cannot handle collections of 10(8)-10(12) compounds typical for DELs...
March 28, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28350958/photo-controlled-sirna-delivery-and-biomarker-triggered-aiegen-emission-by-upconversion-nayf4-yb-3-tm-3-sio2-nanoparticles-for-inducing-and-monitoring-stem-cell-differentiation
#9
Jinming Li, Chris Wai Tung Leung, Dexter Siu Hong Wong, Jianbin Xu, Rui Li, Yueyue Zhao, Chris Yu Yee Yung, Engui Zhao, Benzhong Tang, Liming Bian
Controlling differentiation of stem cell and monitoring the cell differentiation has attracted much research interest since the discovery of stem cells. In this regard, a novel and personalized near-infrared (NIR) light-activated nanoplatform is obtained by encapsulating the photoactivated caged compound (DMNPE/siRNA) and combining a MMP13 cleavaged imaging peptide-tetrapheny-lethene (TPE) unit conjugated with the mesoporous silica coated upconversion nanoparticles (UCNPs) for the remote control of cell differentiation and simultaneously for real-time monitoring of differentiation...
March 28, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28350803/pharmacogenomic-identification-of-small-molecules-for-lineage-specific-manipulation-of-subventricular-zone-germinal-activity
#10
Kasum Azim, Diane Angonin, Guillaume Marcy, Francesca Pieropan, Andrea Rivera, Vanessa Donega, Claudio Cantù, Gareth Williams, Benedikt Berninger, Arthur M Butt, Olivier Raineteau
Strategies for promoting neural regeneration are hindered by the difficulty of manipulating desired neural fates in the brain without complex genetic methods. The subventricular zone (SVZ) is the largest germinal zone of the forebrain and is responsible for the lifelong generation of interneuron subtypes and oligodendrocytes. Here, we have performed a bioinformatics analysis of the transcriptome of dorsal and lateral SVZ in early postnatal mice, including neural stem cells (NSCs) and their immediate progenies, which generate distinct neural lineages...
March 2017: PLoS Biology
https://www.readbyqxmd.com/read/28350492/addressing-stillbirth-in-india-must-include-men
#11
Lisa Roberts, Susanne Montgomery, Gayatri Ganesh, Harinder Pal Kaur, Ratan Singh
BACKGROUND: Millennium Development Goal 4, to reduce child mortality, can only be achieved by reducing stillbirths globally. A confluence of medical and sociocultural factors contribute to the high stillbirth rates in India. The psychosocial aftermath of stillbirth is a well-documented public health problem, though less is known of the experience for men, particularly outside of the Western context. Therefore, men's perceptions and knowledge regarding reproductive health, as well as maternal-child health are important...
March 28, 2017: Issues in Mental Health Nursing
https://www.readbyqxmd.com/read/28350469/synthesis-of-sugar-boronic-acid-derivatives-a-class-of-potential-agents-for-boron-neutron-capture-therapy
#12
Daniela Imperio, Erika Del Grosso, Silvia Fallarini, Grazia Lombardi, Luigi Panza
To date, sugar analogues that contain boronic acids as substitutes for hydroxyl groups are a class of compounds nearly unknown in the literature. The challenging synthesis of two sugar-boronic acid analogues is described, and data are retrieved on their solution behavior, stability, and toxicity. As these compounds were expected to mimic the behavior of carbohydrates, they were tested in regards to their future development as potential boron neutron capture therapy agents.
March 28, 2017: Organic Letters
https://www.readbyqxmd.com/read/28350454/structural-optimizations-of-thieno-3-2-b-pyrrole-derivatives-for-the-development-of-metabolically-stable-inhibitors-of-chikungunya-virus
#13
Kuan Chieh Ching, Thi Ngoc Quy Tran, Siti Naqiah Amrun, Yiu Wing Kam, Lisa F P Ng, Christina Li Lin Chai
Chikungunya virus (CHIKV) is a re-emerging vector-borne alphavirus and there is no approved effective antiviral treatment currently available for CHIKV. We previously reported the discovery of thieno[3,2-b]pyrrole 1b that displayed good antiviral activity against CHIKV infection in vitro. However, it has a short half-life in the presence of human liver microsomes (HLMs) (T1/2 = 2.91 min). Herein, we report further optimization studies in which potential metabolically labile sites on compound 1b were removed or modified, resulting in the identification of thieno[3,2-b]pyrrole 20 and pyrrolo[2,3-d]thiazole 23c possessing up to 17-fold increase in metabolic half-lives in HLMs and good in vivo pharmacokinetic properties...
March 28, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28350449/long-chained-4-aminoquinolines-as-quorum-sensing-inhibitors-in-serratia-marcescens-and-pseudomonas-aeruginosa
#14
Ivana Aleksić, Sandra Šegan, Filip Andric, Mario Zlatović, Ivana Moric, Dejan M Opsenica, Lidija Senerovic
Antibiotic resistance has become serious global threat to public health; therefore, the improved strategies and structurally novel antimicrobials are urgently needed to combat infectious diseases. Here we report a new type of highly potent 4-aminoquinoline derivatives as quorum sensing inhibitors in Serratia marcescens and Pseudomonas aeruginosa, exhibiting weak bactericidal activities (MIC > 400 μM). Through detailed structure-activity study we have identified 7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines (5 and 10) as biofilm formation inhibitors with 50% biofilm inhibition at 69 μM and 63 μM in S...
March 28, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28350446/temporal-shifts-in-poly-and-perfluoroalkyl-substances-pfass-in-north-atlantic-pilot-whales-indicate-large-contribution-of-atmospheric-precursors
#15
Clifton Dassuncao, Xindi C Hu, Xianming Zhang, Rossana Bossi, Maria Dam, Bjarni Mikkelsen, Elsie M Sunderland
Poly- and perfluoroalkyl substances (PFASs) are persistent, bioaccumulative anthropogenic compounds associated with adverse health impacts on humans and wildlife. PFAS production changed in North America and Europe around the year 2000, but impacts on wildlife appear to vary across species and location. Unlike other mammal species, cetaceans lack the enzyme for transforming an important intermediate precursor (perfluorooctane sulfonamide: FOSA), into a prevalent compound in most wildlife (perfluorooctanesulfonate: PFOS)...
March 28, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28350440/identification-of-trypanosoma-brucei-adometdc-inhibitors-using-a-high-throughput-mass-spectrometry-based-assay
#16
Oleg A Volkov, Casey C Cosner, Anthony J Brockway, Martin Kramer, Michael Booker, Shihua Zhong, Ariel Ketcherside, Shuguang Wei, Jamie Longgood, Melissa K McCoy, Thomas E Richardson, Stephen A Wring, Michael Peel, Jeffrey D Klinger, Bruce A Posner, Jef K De Brabander, Margaret A Phillips
Human African trypanosomiasis (HAT) is a fatal infectious disease caused by the eukaryotic pathogen Trypanosoma brucei. Available treatments are difficult to administer and have significant safety issues. S-Adenosylmethionine decarboxylase (AdoMetDC) is an essential enzyme in the parasite polyamine biosynthetic pathway. Previous attempts to develop TbAdoMetDC inhibitors into anti-HAT therapies failed due to poor brain exposure. Here, we describe a large screening campaign of two small-molecule libraries (~400,000 compounds) employing a new high-throughput (~7 s per sample) mass spectrometry-based assay for AdoMetDC activity...
March 28, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28346965/point-of-care-coagulation-tests-monitoring-of-direct-oral-anticoagulants-and-their-reversal-therapy-state-of-the-art
#17
Giacomo E Iapichino, Paolo Bianchi, Marco Ranucci, Ekaterina Baryshnikova
Direct oral anticoagulants (DOACs) exert similar anticoagulant effects to vitamin K antagonists and are increasingly used worldwide. Nevertheless, an evidence-based approach to patients receiving DOACs when any unplanned urgent surgery or bleeding (either spontaneous or traumatic) occurs is still missing. In this review, we investigate the role of point-of-care coagulation tests when other, more specific tests are not available. Indeed, thromboelastography and activated clotting time can detect dabigatran-induced coagulopathy, while their accuracy is limited for apixaban and rivaroxaban, mostly in cases of low drug plasma concentrations...
March 27, 2017: Seminars in Thrombosis and Hemostasis
https://www.readbyqxmd.com/read/28346939/a-b12-dependent-radical-sam-enzyme-involved-in-oxetanocin-a-biosynthesis
#18
Jennifer Bridwell-Rabb, Aoshu Zhong, He G Sun, Catherine L Drennan, Hung-Wen Liu
Oxetanocin A (OXT-A) is a potent antitumour, antiviral and antibacterial compound. Biosynthesis of OXT-A has been linked to a plasmid-borne Bacillus megaterium gene cluster that contains four genes: oxsA, oxsB, oxrA and oxrB. Here we show that both the oxsA and oxsB genes are required for the production of OXT-A. Biochemical analysis of the encoded proteins, a cobalamin (Cbl)-dependent S-adenosylmethionine (AdoMet) radical enzyme, OxsB, and an HD-domain phosphohydrolase, OxsA, reveals that OXT-A is derived from a 2'-deoxyadenosine phosphate in an OxsB-catalysed ring contraction reaction initiated by hydrogen atom abstraction from C2'...
March 27, 2017: Nature
https://www.readbyqxmd.com/read/28346909/bioaugmentaton-in-technosols-created-in-abandoned-pyritic-tailings-can-contribute-to-enhance-soil-c-sequestration-and-plant-colonization
#19
Raúl Zornoza, Melisa Gómez-Garrido, Silvia Martínez-Martínez, María Dolores Gómez-López, Ángel Faz
Creation of Technosols in combination with phytostabilization may be a sustainable strategy to minimize the environmental and human health hazards derived from mine tailings. Bioaugmentation can facilitate plant establishment and growth for efficient phytostabilization. In order to assess if bioaugmentation can increase soil quality and fertility, decrease metal(loid) mobility and accelerate plant colonization, a one-year field experiment was designed with creation of Technosols in two tailings ponds with different pH (acidic (AT) and neutral (NT)), with addition of marble waste (MaW) and two organic materials (pig manure (PM) and sewage sludge (SS), without or with inoculation of effective microorganisms (EM) at three rates...
March 24, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28346882/determination-of-prodrug-treosulfan-and-its-biologically-active-monoepoxide-in-rat-plasma-liver-lungs-kidneys-muscle-and-brain-by-hplc-esi-ms-ms-method
#20
Michał Romański, Anna Kasprzyk, Artur Teżyk, Agnieszka Widerowska, Czesław Żaba, Franciszek Główka
A prodrug treosulfan (TREO) is currently investigated in clinical trials for conditioning prior to hematopoietic stem cell transplantation. Bioanalysis of TREO and its active derivatives, monoepoxide (S,S-EBDM) and diepoxide, in plasma and urine underlay the pharmacokinetic studies of these compounds but cannot explain an organ pharmacological action or toxicity. Recently, distribution of TREO and S,S-EBDM into brain, cerebrospinal fluid, and aqueous humor of the eye has been investigated in animal models and the obtained results presented clinical relevance...
March 18, 2017: Journal of Pharmaceutical and Biomedical Analysis
keyword
keyword
53363
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"