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https://www.readbyqxmd.com/read/28340413/design-synthesis-and-biological-evaluation-of-novel-coumarin-based-benzamides-as-potent-histone-deacetylase-inhibitors-and-anticancer-agents
#1
Tooba Abdizadeh, Mohammad Reza Kalani, Khalil Abnous, Zahra Tayarani-Najaran, Bibi Zahra Khashyarmanesh, Rahman Abdizadeh, Razieh Ghodsi, Farzin Hadizadeh
Histone deacetylases (HDACs) are attractive therapeutic targets for the treatment of cancer and other diseases. It has four classes (I-IV), among them especially class I isozyme are involved in promoting tumor cells proliferation, angiogenesis, differentiation, invasion and metastasis and also viable targets for cancer therapeutics. A novel series of coumarin-based benzamides was designed and synthesized as HDAC inhibitors. The cytotoxic activity of the synthesized compounds (8a-u) was evaluated against six human cancer cell lines including HCT116, A2780, MCF7, PC3, HL60 and A549 and a single normal cell line (Huvec)...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340411/synthesis-and-biological-evaluation-of-novel-chalcone-derivatives-as-a-new-class-of-microtubule-destabilizing-agents
#2
Xiaochao Huang, Rizhen Huang, Lingxue Li, Shaohua Gou, Hengshan Wang
A series of novel chalcone derivatives were designed and synthesized as potential antitumor agents. Structures of target molecules were confirmed by (1)H NMR, (13)C NMR and HR-MS, and evaluated for their in vitro anti-proliferative activities using MTT assay. Among them, compound 12k displayed potent activity against the test tumor cell lines including multidrug resistant human cancer lines, with the IC50 values ranged from 3.75 to 8.42 μM. In addition, compound 12k was found to induce apoptosis in NCI-H460 cells via the mitochondrial pathway, including an increase of the ROS level, loss of mitochondrial membrane potential, release of cytochrome c, down-regulation of Bcl-2, up-regulation of Bax, activation of caspase-9 and caspase-3, respectively...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340404/synthesis-in-vitro-antiproliferative-activity-and-kinase-profile-of-new-benzimidazole-and-benzotriazole-derivatives
#3
Konrad Chojnacki, Patrycja Wińska, Katarzyna Skierka, Monika Wielechowska, Maria Bretner
Protein kinase 2 (CK2), a member of the serine/threonine kinase family, has been established as a promising target in anticancer therapy. New derivatives of known CK2 inhibitors 4,5,6,7-tetrabromo-1H-benzimidazole (TBBi) and 4,5,6,7-tetrabromo-1H-benzotriazole (TBBt) bearing azide or substituted triazole groups were synthesized. Their influence on the activity of human recombinant CK2α and cytotoxicity against normal and cancer cell lines were evaluated. TBBi derivatives with triazole substituted with carboxyl substituent (7 and 10) exhibited the most potent inhibitory activity against CK2 with Ki value in the range of 1...
March 16, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28340268/is-differential-expression-of-p16ink4a-based-on-the-classification-of-uterine-smooth-muscle-tumors-associated-with-a-different-prognosis-a-meta-analysis
#4
H Y Cao, S Yang, S Wang, L Y Deng, J Y Lou
We conducted a meta-analysis to examine p16INK4a expression in uterine smooth muscle tumors (USMTs). Although the prognostic value of tumor suppressor p16INK4a has been elucidated in a variety of cancers and precancerous lesions, its role in USMTs is not well established. We searched PubMed, Web of Science, and Embase for publication son p16INK4a expression in USMTs. Strict inclusion and exclusion criteria were imposed. Risk ratios (RRs) with 95% confidence intervals (95%CIs) were calculated to assess the strength of association...
March 22, 2017: Genetics and Molecular Research: GMR
https://www.readbyqxmd.com/read/28340204/changes-in-pain-and-muscle-architecture-in-colon-cancer-survivors-after-a-lumbopelvic-exercise-program-a-secondary-analysis-of-a-randomized-controlled-trial
#5
Irene Cantarero-Villanueva, Antonio I Cuesta-Vargas, Mario Lozano-Lozano, Carolina Fernández-Lao, Antonio Fernández-Pérez, Noelia Galiano-Castillo
Objective.:  To investigate the efficacy of an eight-week lumbopelvic stabilization program (CO-CUIDATE) for colon cancer survivors. Design.:  A secondary analysis of a randomized controlled clinical trial. Settings.:  A blinded, trained researcher performed the end point assessments for pain (Pressure Pain Threshold and Brief Pain Inventory) and muscle architecture (ultrasound imaging measurements). Subjects.:  Forty-six colon cancer survivors who were assigned to the CO-CUIDATE group or usual care group...
March 6, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28339844/intensity-modulated-radiotherapy-using-two-static-ports-of-tomotherapy-for-breast-cancer-after-conservative-surgery-dosimetric-comparison-with-other-treatment-methods-and-3-year-clinical-results
#6
Aiko Nagai, Yuta Shibamoto, Masanori Yoshida, Koji Inoda, Yuzo Kikuchi
This study investigated the differences in dose-volume parameters for the breast and normal tissues during TomoDirectTM (TD) intensity-modulated radiation therapy (IMRT), TD-3D conformal radiotherapy (3DCRT) and 3DCRT plans, all using two beams, and analyzed treatment outcomes of two-beam TD-IMRT for breast cancer after breast-conserving surgery. Between August 2011 and January 2015, 152 patients were treated using two-beam TD-IMRT with 50 Gy/25 fractions. Among them, 20 patients with left-sided breast cancer were randomly chosen, and two-beam TD-IMRT, TD-3DCRT and 3DCRT plans were created for each patient...
February 23, 2017: Journal of Radiation Research
https://www.readbyqxmd.com/read/28339746/in-vitro-cytotoxic-and-ace-inhibitory-activities-of-promod-278p-hydrolysate-of-ovotransferrin-from-chicken-egg-white
#7
S H Moon, J H Lee, J H Kim, H-D Paik, D U Ahn
Peptides released from egg proteins via enzymatic hydrolysis show various bioactivities such as antimicrobial, antioxidant, antihypertensive, and immunomodulatory properties. The objective of this study was to investigate the cytotoxic and Angiotensin Converting Enzyme (ACE)-inhibitory activities of ovotransferrin and its promod 278P enzyme hydrolysate. Ovotransferrin from egg white was hydrolyzed using promod 278P at 45°C for 3 hours. Using the MTT assay, the cytotoxicity of ovotransferrin and promod 278P hydrolysate of ovotransferrin were evaluated in human cancer cell lines of various tissue origins...
February 22, 2017: Poultry Science
https://www.readbyqxmd.com/read/28339723/leveraging-molecular-datasets-for-biomarker-based-clinical-trial-design-in-glioblastoma
#8
Shyam K Tanguturi, Lorenzo Trippa, Shakti H Ramkissoon, Kristine Pelton, David Knoff, David Sandak, Neal I Lindeman, Azra H Ligon, Rameen Beroukhim, Giovanni Parmigiani, Patrick Y Wen, Keith L Ligon, Brian M Alexander
Background.: Biomarkers can improve clinical trial efficiency, but designing and interpreting biomarker-driven trials require knowledge of relationships among biomarkers, clinical covariates, and endpoints. We investigated these relationships across genomic subgroups of glioblastoma (GBM) within our institution (DF/BWCC), validated results in The Cancer Genome Atlas (TCGA), and demonstrated potential impacts on clinical trial design and interpretation. Methods.: We identified genotyped patients at DF/BWCC, and clinical associations across 4 common GBM genomic biomarker groups were compared along with overall survival (OS), progression-free survival (PFS), and survival post-progression (SPP)...
February 20, 2017: Neuro-oncology
https://www.readbyqxmd.com/read/28339311/lung-rads-category-4x-does-it-improve-prediction-of-malignancy-in-subsolid-nodules
#9
Kaman Chung, Colin Jacobs, Ernst T Scholten, Jin Mo Goo, Helmut Prosch, Nicola Sverzellati, Francesco Ciompi, Onno M Mets, Paul K Gerke, Mathias Prokop, Bram van Ginneken, Cornelia M Schaefer-Prokop
Purpose To evaluate the added value of Lung CT Screening Reporting and Data System (Lung-RADS) assessment category 4X over categories 3, 4A, and 4B for differentiating between benign and malignant subsolid nodules (SSNs). Materials and Methods SSNs on all baseline computed tomographic (CT) scans from the National Lung Cancer Trial that would have been classified as Lung-RADS category 3 or higher were identified, resulting in 374 SSNs for analysis. An experienced screening radiologist volumetrically segmented all solid cores and located all malignant SSNs visible on baseline scans...
March 24, 2017: Radiology
https://www.readbyqxmd.com/read/28339196/discovery-of-a-small-molecule-degrader-of-bromodomain-and-extra-terminal-bet-proteins-with-picomolar-cellular-potencies-and-capable-of-achieving-tumor-regression
#10
Bing Zhou, Jiantao Hu, Fuming Xu, Zhuo Chen, Longchuan Bai, Ester Fernandez-Salas, Mei Lin, Liu Liu, Chao-Yie Yang, Yujun Zhao, Donna McEachern, Sally Przybranowski, Bo Wen, Duxin Sun, Shaomeng Wang
The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic "readers" and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-molecule BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation. Herein, we present our design, synthesis, and evaluation of a new class of PROTAC BET degraders...
March 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28336434/vav1-expression-is-increased-in-esophageal-squamous-cell-carcinoma-and-indicates-poor-prognosis
#11
Xiaolei Zhu, Huan Jin, Ziwei Xia, Xianxian Wu, Mingjian Yang, Hongdian Zhang, Xiaobin Shang, Runfen Cheng, Zhongli Zhan, Zhentao Yu
Recently, Vav1 has been suggested to play an essential role in the progression of human cancers. However, the correlation between Vav1 expression and prognosis of esophageal squamous cell carcinoma (ESCC) is still unknown. The aim of this study was to investigate Vav1 expression and its prognostic value in ESCC. The expression of Vav1 was detected by real-time quantitative reverse transcription polymerase chain reaction (qRT-PCR) and Western blotting in ESCC tissues and matched nontumorous tissues. Immunohistochemistry (IHC) was carried out to detect Vav1 expression in paraffin samples from 112 primary ESCC patients...
March 20, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28335559/the-optimization-and-characterization-of-an-rna-cleaving-fluorogenic-dnazyme-probe-for-mda-mb-231-cell-detection
#12
Pengcheng Xue, Shengnan He, Yu Mao, Long Qu, Feng Liu, Chunyan Tan, Yuyang Jiang, Ying Tan
Breast cancer is one of the most frequently diagnosed cancers in females worldwide and lacks specific biomarkers for early detection. In a previous study, we obtained a selective RNA-cleaving Fluorogenic DNAzyme (RFD) probe against MDA-MB-231 cells, typical breast cancer cells, through the systematic evolution of ligands by exponential process (SELEX). To improve the performance of this probe for actual application, we carried out a series of optimization experiments on the pH value of a reaction buffer, the type and concentration of cofactor ions, and sequence minimization...
March 21, 2017: Sensors
https://www.readbyqxmd.com/read/28335512/symptoms-relevant-to-surveillance-for-ovarian-cancer
#13
Robert M Ore, Lauren Baldwin, Dylan Woolum, Erika Elliott, Christiaan Wijers, Chieh-Yu Chen, Rachel W Miller, Christopher P DeSimone, Frederick R Ueland, Richard J Kryscio, John R van Nagell, Edward J Pavlik
To examine how frequently and confidently healthy women report symptoms during surveillance for ovarian cancer. A symptoms questionnaire was administered to 24,526 women over multiple visits accounting for 70,734 reports. A query of reported confidence was included as a confidence score (CS). Chi square, McNemars test, ANOVA and multivariate analyses were performed. 17,623 women completed the symptoms questionnaire more than one time and >9500 women completed it more than one four times for >43,000 serially completed questionnaires...
March 20, 2017: Diagnostics
https://www.readbyqxmd.com/read/28335509/novel-diagnostic-and-predictive-biomarkers-in-pancreatic-adenocarcinoma
#14
REVIEW
John C Chang, Madappa Kundranda
Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal disease for a multitude of reasons including very late diagnosis. This in part is due to the lack of understanding of the biological behavior of PDAC and the ineffective screening for this disease. Significant efforts have been dedicated to finding the appropriate serum and imaging biomarkers to help early detection and predict response to treatment of PDAC. Carbohydrate antigen 19-9 (CA 19-9) has been the most validated serum marker and has the highest positive predictive value as a stand-alone marker...
March 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28335504/diagnosis-of-breast-cancer-tissues-using-785-nm-miniature-raman-spectrometer-and-pattern-regression
#15
Qingbo Li, Can Hao, Zhi Xu
For achieving the development of a portable, low-cost and in vivo cancer diagnosis instrument, a laser 785 nm miniature Raman spectrometer was used to acquire the Raman spectra for breast cancer detection in this paper. However, because of the low spectral signal-to-noise ratio, it is difficult to achieve high discrimination accuracy by using the miniature Raman spectrometer. Therefore, a pattern recognition method of the adaptive net analyte signal (NAS) weight k-local hyperplane (ANWKH) is proposed to increase the classification accuracy...
March 19, 2017: Sensors
https://www.readbyqxmd.com/read/28335450/assessment-of-radioactive-materials-and-heavy-metals-in-the-surface-soil-around-the-bayanwula-prospective-uranium-mining-area-in-china
#16
Haribala Bai, Bitao Hu, Chengguo Wang, Shanhu Bao, Gerilemandahu Sai, Xiao Xu, Shuai Zhang, Yuhong Li
The present work is the first systematic and large scale study on radioactive materials and heavy metals in surface soil around the Bayanwula prospective uranium mining area in China. In this work, both natural and anthropogenic radionuclides and heavy metals in 48 surface soil samples were analyzed using High Purity Germanium (HPGe) γ spectrometry and inductively coupled plasma-mass spectrometry (ICP-MS). The obtained mean activity concentrations of (238)U, (226)Ra, (232)Th, (40)K, and (137)Cs were 25.81 ± 9...
March 14, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28335402/2-hydroxymelatonin-a-predominant-hydroxylated-melatonin-metabolite-in-plants-shows-antitumor-activity-against-human-colorectal-cancer-cells
#17
Yi Yang, Rui Zhou, So-Yeon Park, Kyoungwhan Back, Woo Kyun Bae, Kyung Keun Kim, Hangun Kim
2-Hydroxymelatonin is a predominant hydroxylated melatonin metabolite in plants. To investigate whether it has potent cytotoxic effects on colorectal cancer cells, four colorectal cancer cell lines, Caco2, HCT116, DLD1, and CT26, were treated with 2-hydroxymelatonin and melatonin. 2-Hydroxymelatonin had a much lower IC50 value than melatonin in the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The cytotoxic effect of 2-hydroxymelatonin was much stronger than that of melatonin at high concentrations (1000 or 2000 μM) in HCT116, DLD1, and CT26 cells, but only at intermediate concentrations (250 or 500 μM) in Caco2 cells...
March 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335391/new-metabolites-and-bioactive-chlorinated-benzophenone-derivatives-produced-by-a-marine-derived-fungus-pestalotiopsis-heterocornis
#18
Hui Lei, Xiuping Lin, Li Han, Jian Ma, Qingjuan Ma, Jialiang Zhong, Yonghong Liu, Tiemin Sun, Jinhui Wang, Xueshi Huang
Four new compounds, including two isocoumarins, pestaloisocoumarins A and B (1, 2), one sesquiterpenoid degradation, isopolisin B (4), and one furan derivative, pestalotiol A (5), together with one known isocoumarin, gamahorin (3), and three chlorinated benzophenone derivatives, pestalachloride B (6), pestalachloride E (7) and a mixture of pestalalactone atropisomers (8a/8b), were isolated from a culture of the fungus Pestalotiopsis heterocornis associated with sponge Phakellia fusca. These new chemical structures were established using NMR and MS spectroscopic data, as well as single-crystal X-ray crystallographic analysis and CD Cotton effects...
March 13, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28335242/targeting-and-photodynamic-killing-of-cancer-cell-by-nitrogen-doped-titanium-dioxide-coupled-with-folic-acid
#19
Jin Xie, Xiaobo Pan, Mengyan Wang, Longfang Yao, Xinyue Liang, Jiong Ma, Yiyan Fei, Pei-Nan Wang, Lan Mi
Titanium dioxide (TiO₂) has attracted wide attention as a potential photosensitizer (PS) in photodynamic therapy (PDT). However, bare TiO₂ can only be excited by ultraviolet illumination, and it lacks specific targeting ligands, which largely impede its application. In our study, we produced nitrogen-doped TiO₂ and linked it with an effective cancer cell targeting agent, folic acid (FA), to obtain N-TiO₂-FA nanoconjugates. Characterization of N-TiO₂-FA included Zeta potential, absorption spectra and thermogravimetric analysis...
June 14, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28335081/the-impact-of-body-mass-index-and-nuclear-%C3%AE-catenin-on-survival-in-locally-advanced-rectal-cancer-treated-with-preoperative-radiochemotherapy
#20
Jaime Gomez-Millan, Maria Isabel Queipo, Maria Del Mar Delgado, Lidia Perez-Villa, Alicia Roman, Fernando De la Portilla, Esperanza Torres, Vanessa De Luque, Eloisa Bayo, Jose Antonio Medina
BACKGROUND AND OBJECTIVE: We examined the prognostic value of obesity and nuclear β-catenin in patients with locally advanced rectal cancer. METHODS: We prospectively recruited a total of 98 eligible patients with locally advanced cancer for preoperative radiochemotherapy followed by total mesorectal excision. Patients' height and weight were reaorded before radiochemotherapy, and the immunohistochemical expression of nuclear β-catenin was analyzed. Disease-free survival (DFS) was analyzed using the Kaplan-Meier method and a Cox regression model was employed for the multivariate analysis...
March 2017: Journal of Surgical Oncology
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