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https://www.readbyqxmd.com/read/28324785/-ub006-a-new-fatty-acid-synthase-inhibitor-and-cytotoxic-agent-without-anorexic-side-effects
#1
Kamil Makowski, Joan Francesc Mir, Paula Mera, Xavier Ariza, Guillermina Asins, Fausto G Hegardt, Laura Herrero, Jordi García, Dolors Serra
C75 is a synthetic anticancer drug that inhibits fatty acid synthase (FAS) and shows a potent anorexigenic side effect. In order to find new cytotoxic compounds that do not impact food intake, we synthesized a new family of C75 derivatives. The most promising anticancer compound among them was UB006 ((4SR,5SR)-4-(hydroxymethyl)-3-methylene-5-octyldihydrofuran-2(3H)-one). The effects of this compound on cytotoxicity, food intake and body weight were studied in UB006 racemic mixture and in both its enantiomers separately...
March 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28324784/an-in%C3%A2-vivo-active-1-2-5-oxadiazole-pt-ii-complex-a-promising-anticancer-agent-endowed-with-stat3-inhibitory-properties
#2
Federica Porta, Giorgio Facchetti, Nicola Ferri, Arianna Gelain, Fiorella Meneghetti, Stefania Villa, Daniela Barlocco, Daniela Masciocchi, Akira Asai, Nao Miyoshi, Silvia Marchianò, Byoung-Mog Kwon, Yena Jin, Valentina Gandin, Cristina Marzano, Isabella Rimoldi
New Pt(II) complexes (Pt-1-3) bearing 1,2,5-oxadiazole ligands (1-3) were synthesized, characterized and evaluated for their ability to disrupt STAT3 dimerization. Ligand 3·HCl showed cytotoxic effects on HCT-116 cells (IC50 = 95.2 μM) and a selective ability to interact with STAT3 (IC50 = 8.2 μM) versus STAT1 (IC50 > 30 μM). Its corresponding platinum complex Pt-3 exhibited an increased cytotoxicity (IC50 = 18.4 μM) and a stronger interaction with STAT3 (IC50 = 1.4 μM), leading to inhibition of its signaling pathway...
March 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28324660/single-and-combination-drug-screening-with-aqueous-biphasic-tumor-spheroids
#3
Pradip Shahi Thakuri, Hossein Tavana
Spheroids of cancer cells represent a physiologic model of solid tumors for cancer drug screening. Despite this known benefit, difficulties with generating large quantities of uniformly sized spheroids in standard plates, individually addressing spheroids with drug compounds, and quantitatively analyzing responses of cancer cells have hindered the use of spheroids in high-throughput screening applications. Recently, we addressed this challenge by using an aqueous two-phase system technology to generate a spheroid within an aqueous drop immersed in a second, immiscible aqueous phase...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28324509/human-telomeric-g-quadruplex-structures-and-g-quadruplex-interactive-compounds
#4
Clement Lin, Danzhou Yang
G-quadruplexes are noncanonical secondary structures formed in DNA sequences containing consecutive runs of guanines. It has been shown that the 3' G-rich single-stranded overhangs of human telomeres can form G-quadruplex structures, and the human telomeric DNA G-quadruplexes are considered attractive targets for anticancer drugs. G-quadruplex-interactive compounds have been shown to inhibit telomerase access as well as telomere capping. Nuclear magnetic resonance (NMR) spectroscopy is a powerful method in determining the G-quadruplex structures under physiologically relevant conditions...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28324320/tailoring-the-properties-of-mpeg-plla-nanoparticles-for-better-encapsulation-and-tuned-release-of-the-hydrophilic-anticancer-drug
#5
Sachin S Surwase, Neha M Munot, Bhaskar B Idage, Susheela B Idage
Gemcitabine is used as a first-line drug for treating many solid tumours. However, it suffers from a major drawback of strong side effects and short plasma half-life because of degradation by enzyme when administered intravenously. Polyesters and copolyesters are the most widely used and preferred class of biodegradable polymer. In the present work, efforts have been made to prepare poly(ethylene glycol) monomethoxy ether-poly(L-lactide) (mPEG-PLLA), a biodegradable amphiphilic copolymer with a view to improve the entrapment and tuned release of hydrophilic drug gemcitabine...
March 21, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28323527/design-synthesis-and-anticancer-evaluation-of-novel-pyrazole-pyrazolo-3-4-d-pyrimidine-and-their-glycoside-derivatives
#6
Ibrahim F Nassar, Ahmed F El Farargy, Fathy M Abdelrazek, Nasser S M Ismail
The chalcone derivatives 3a,b were cyclized upon reaction with thiourea to give the pyrazolo[3,4-d]pyrimidine derivatives 5a,b. Condensation of 5a,b and their hydrazide derivatives 8a,b with cyclic and acyclic glucose gave the condensed S- and N-glycosides 7a,b and 9a,b, respectively. Reaction of 3b with ethyl cyanoacetate followed by reaction with cyclic glucose afforded a mixture of the O- and/or N-glycoside isomers 12 and 13, respectively. The pyrazolo[3,4-c]pyrazole derivative 14 was also obtained from the reaction of 3b with hydrazine hydrate...
March 21, 2017: Nucleosides, Nucleotides & Nucleic Acids
https://www.readbyqxmd.com/read/28323486/enterolactone-induces-g1-phase-cell-cycle-arrest-in-nonsmall-cell-lung-cancer-cells-by-downregulating-cyclins-and-cyclin-dependent-kinases
#7
Shireen Chikara, Kaitlin Lindsey, Harsharan Dhillon, Sujan Mamidi, Jeffrey Kittilson, Melpo Christofidou-Solomidou, Katie M Reindl
Flaxseed is a rich source of the plant lignan secoisolariciresinol diglucoside (SDG), which is metabolized into mammalian lignans enterodiol (ED) and enterolactone (EL) in the digestive tract. The anticancer properties of these lignans have been demonstrated for various cancer types, but have not been studied for lung cancer. In this study, we investigated the anticancer effects of EL for several nonsmall cell lung cancer (NSCLC) cell lines of various genetic backgrounds. EL inhibited the growth of A549, H441, and H520 lung cancer cells in concentration- and time-dependent manners...
March 21, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28320095/dt-13-a-saponin-monomer-13-of-the-dwarf-lilyturf-tuber-synergized-with-vinorelbine-to-induce-mitotic-arrest-via-activation-of-erk-signaling-pathway-in-nci-h1299-cells
#8
Hongyang Li, Li Sun, Hang Li, Xiaodan Lv, Herve Semukunzi, Ruiming Li, Jun Yu, Shengtao Yuan, Sensen Lin
Vinorelbine (NVB) is a semi-synthetic vinca alkaloid that is approved for the clinical therapy of lung cancer. However, the clinical application of NVB was limited because of the acquisition of resistance and inacceptable toxicity. Therefore, it is of great interest to develop low-cytotoxic drugs that can synergize with NVB. DT-13, a saponin monomer 13 of the Dwarf lilyturf tuber, showed inhibitory effects on tumor metastasis and angiogenesis in the previous studies. Here, we found that DT-13 combined with NVB exhibited synergistic effect to inhibit the cell proliferation in human lung cancer NCI-H1299 cells rather than human embryonic lung fibroblasts WI-38...
March 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28320088/flower-extract-of-allium-atroviolaceum-triggered-apoptosis-activated-caspase-3-and-down-regulated-antiapoptotic-bcl-2-gene-in-hela-cancer-cell-line
#9
Somayeh Khazaei, Vasudevan Ramachandran, Roslida Abdul Hamid, Norhaizan Mohd Esa, Ali Etemad, Sara Moradipoor, Patimah Ismail
Cervical cancer accounts for the second most frequent cancer and also third leading cause of cancer mortality (15%) among women worldwide. The major problems of chemotherapeutic treatment in cervical cancer are non-specific cytotoxicity and drug resistance. Plant-derived products, known as natural therapies, have been used for thousands of years in cancer treatment with a very low number of side effects. Allium atroviolaceum is a species in the genus Allium and Liliaceae family, which could prove to have beneficial effects on cancer treatment, although there is a lack of corresponding attention...
March 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28320043/effects-of-ranolazine-in-a-model-of-doxorubicin-induced-left-ventricle-diastolic-dysfunction
#10
Donato Cappetta, Grazia Esposito, Raffaele Coppini, Elena Piegari, Rosa Russo, Loreta Pia Ciuffreda, Alessia Rivellino, Lorenzo Santini, Concetta Rafaniello, Cristina Scavone, Francesco Rossi, Liberato Berrino, Konrad Urbanek, Antonella De Angelis
BACKGROUND AND PURPOSE: Doxorubicin (DOXO) is a highly effective anticancer drug but its clinical application is impeded by cardiotoxicity. Asymptomatic diastolic dysfunction can be the earliest manifestation of DOXO cardiotoxicity. Therefore, a search for therapeutic intervention that can interfere with early manifestations and possibly prevent late cardiotoxicity is warranted. Increased DOXO-dependent reactive oxygen species may explain, in part, Ca(2+) and Na(+) overload that contributes to diastolic dysfunction and development of heart failure...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28319807/targeting-nf-kappa-b-signaling-by-artesunate-restores-sensitivity-of-castrate-resistant-prostate-cancer-cells-to-antiandrogens
#11
Jessica J Nunes, Swaroop K Pandey, Anjali Yadav, Sakshi Goel, Bushra Ateeq
Androgen deprivation therapy (ADT) is the most preferred treatment for men with metastatic prostate cancer (PCa). However, the disease eventually progresses and develops resistance to ADT in majority of the patients, leading to the emergence of metastatic castration-resistant prostate cancer (mCRPC). Here, we assessed artesunate (AS), an artemisinin derivative, for its anticancer properties and ability to alleviate resistance to androgen receptor (AR) antagonists. We have shown AS in combination with bicalutamide (Bic) attenuates the oncogenic properties of the castrate-resistant (PC3, 22RV1) and androgen-responsive (LNCaP) PCa cells...
March 16, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28319647/cancer-specific-intracellular-reductive-activation-of-anticancer-pt-iv-prodrugs
#12
Andriy Mokhir, Viktor Reshetnikov, Steffen Daum
Since cellular uptake of anticancer Pt(II)- and Pt(IV)-drugs occurs via different mechanisms, the latter ones can exhibit substantial activity towards cells, which have either intrinsic or acquired resistance towards Pt(II)-drugs. However, this positive effect is diminished due to reductive activation of Pt(IV)-drugs in extracellular space that can be one of the reasons why they were not yet approved for clinical use despite over 60 clinical trials conducted worldwide. Herein we suggest a solution to this problem by achieving highly specific intracellular versus extracellular prodrug reduction...
March 20, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28319409/investigation-of-anticarcinogenic-and-antioxidant-effects-of-methylimidazole
#13
M Norizadeh Tazehkand, O Hajipour, F Moridikia, A Moridikia, E Valipour, M B Yilmaz, M Topaktas
4-methylimidazole is widely used in pharmaceuticals, photographic and agricultural chemicals. The substance is extensively found in many human and animals foods. In this research, anticancer effect of the 4-MEI was studded using MTT test using MCF-7 cell line. Effect of the 4-MEI on apoptosis or necrosis was analyzed by DNA fragmentation assay using Swiss Albino rats as a model organism. Antioxidant effect of the substance was investigated by assaying protective effect of the substance on circular plasmid DNA against H2O2 as an oxidative agent...
2017: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/28317412/bioactivity-guided-isolation-of-cytotoxic-terpenoids-and-steroids-from-premna-serratifolia
#14
Mahesh Biradi, Kirankumar Hullatti
CONTEXT: Despite several phytochemical studies of Premna serratifolia Linn. (Verbenaceae), the isolation of active constituents of this plant remains to be explored. OBJECTIVE: The study isolates cytotoxic terpenoids and steroids from the leaves of Premna serratifolia. MATERIALS AND METHODS: Unsaponifiable matter of hexane soluble fraction obtained from methanol extract was subjected to isolation by column chromatography and preparative TLC...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28317320/differential-in-vitro-antitumor-activity-of-essential-oil-of-lippia-citriodora-from-different-regions-in-morocco
#15
Moulay Ali Oukerrou, Mounir Tilaoui, Hassan Ait Mouse, Najat Bouchmaa, Abdelmajid Zyad
The aim of this work was to investigate the in vitro anticancer effect of the essential oil of dried leaves of Lippia citriodora (H.B. & K.) harvested in different regions of Morocco. This effect was evaluated against the P815 murine mastocytoma cell line using the MTT assay. Interestingly, this work demonstrated for the first time that these essential oils exhibited a strong cytotoxic activity against the P815 cell line, with IC50 values ranging from 7.75 μg/ml to 13.25 μg/ml. This cytotoxicity began early and increased in a dose and time dependent manner...
March 19, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28317028/mycobacterial-caseinolytic-protease-gene-regulator-clgr-is-a-substrate-of-caseinolytic-protease
#16
Yoshiyuki Yamada, Thomas Dick
The mycobacterial caseinolytic protease ClpP1P2 is a degradative protease that recently gained interest as a genetically and pharmacologically validated drug target for tuberculosis. The first whole-cell active ClpP1P2 inhibitor, the human proteasome inhibitor bortezomib, is currently undergoing lead optimization to introduce selectivity for the bacterial target. How inhibition of ClpP1P2 translates into whole-cell antimicrobial activity is little understood. Previous work has shown that the caseinolytic protease gene regulator ClgR is an activator of the clpP1P2 genes and also suggested that this transcription factor may be a substrate of the protease...
March 2017: MSphere
https://www.readbyqxmd.com/read/28316375/torilin-inhibits-inflammation-by-limiting-tak1-mediated-map-kinase-and-nf-%C3%AE%C2%BAb-activation
#17
Mehari Endale, Tae-Hwan Kim, Yi-Seong Kwak, Na-Mi Kim, Seung-Hyung Kim, Jae Youl Cho, Bong-Sik Yun, Man-Hee Rhee
Torilin, a sesquiterpene isolated from the fruits of Torilis japonica, has shown antimicrobial, anticancer, and anti-inflammatory properties. However, data on the mechanism of torilin action against inflammation is limited. This study aimed at determining the anti-inflammatory property of torilin in LPS-induced inflammation using in vitro model of inflammation. We examined torilin's effect on expression levels of inflammatory mediators and cytokines in LPS-stimulated RAW 264.7 macrophages. The involvement of NF-kB and AP-1, MAP kinases, and adaptor proteins were assessed...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28316129/cognitive-compensatory-processes-of-older-clinically-fit-patients-with-hematologic-malignancies-undergoing-chemotherapy-a-longitudinal-cohort-study
#18
Yves Libert, Cindy Borghgraef, Yves Beguin, Nicole Delvaux, Martine Devos, Chantal Doyen, Stéphanie Dubruille, Anne-Marie Etienne, Aurore Liénard, Isabelle Merckaert, Christine Reynaert, Jean-Louis Slachmuylder, Nicole Straetmans, Eric Van Den Neste, Dominique Bron, Darius Razavi
OBJECTIVE: Despite the well-known negative impacts of cancer and anticancer therapies on cognitive performance, little is known about the cognitive compensatory processes of older patients with cancer. This study was designed to investigate the cognitive compensatory processes of older, clinically-fit patients with hematologic malignancies undergoing chemotherapy. METHODS: We assessed 89 consecutive patients (age ≥ 65 years) without severe cognitive impairment and 89 age-, sex-, and education level-matched healthy controls...
March 18, 2017: Psycho-oncology
https://www.readbyqxmd.com/read/28316026/zebrafish-as-a-model-to-evaluate-peptide-related-cancer-therapies
#19
REVIEW
Austin Y Shull, Chien-An A Hu, Yong Teng
Peptide-derived drug discovery has experienced a remarkable resurgence in the past decade since the failure of small-molecule modulators to effectively access the large binding surfaces of intracellular protein-protein interactions as well as "undruggable" residues of certain disease-driving proteins. However, the effectiveness of peptide-based cancer therapies is being questioned in light of declines in pharmaceutical R&D efficiency. As a model of whole organism, zebrafish provide a means to develop promising peptide and protein anticancer agents in an informative, cost-effective and time-efficient manner, which also allows for surveying mechanisms of drug action and optimization of drug delivery system...
March 18, 2017: Amino Acids
https://www.readbyqxmd.com/read/28315545/oral-anticancer-agents-an-intervention-to-promote-medication-adherence-and-symptom-management%C3%A2
#20
Sandra L Spoelstra, Alla Sikorskii, Atreyee Majumder, Peggy S Burhenn, Monica Schueller, Barbara Given
Symptom burden and poor adherence to oral anticancer agents remain significant clinical problems. This study examined feasibility, preliminary efficacy, and satisfaction with ADHERE, a nurse practitioner intervention that promotes symptom management and adherence among patients prescribed oral agents. The intervention group (which received one semistructured, face-to-face session followed by three weekly telephone sessions using motivational interviewing, brief cognitive-behavioral therapy, and a toolkit to promote self-management) had significantly lower symptom severity postintervention...
April 1, 2017: Clinical Journal of Oncology Nursing
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