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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28270083/ferulenol-a-sesquiterpene-coumarin-induce-apoptosis-via-mitochondrial-dysregulation-in-lung-cancer-induced-by-benzo-a-pyrene-involvement-of-bcl2-protein
#1
Nesrine Lariche, Lahouel Mesbah, Lamia Benguedouar, Amar Zellagui
BACKGROUND: Ferulenol, a sesquiterpene coumarin, was extracted from "Ferula vesceritensis" and possesses pro-oxidative and anticancer effects in different types of cancer. OBJECTIVE: The objective of this study is to determine whether ferulenol has an anticancer effect by regulation the Bcl2 protein expression in lung cancer induced by benzo[a]pyrene in Wistar rats. METHODS: Rats in group 1 have received, intraperitoneally, olive oil and considered as controls, animals of group 2 were treated with 100 mg/kg of benzo[a]pyrene intraperitoneally in order to induce lung cancer for 24 weeks, the 3rd groups of rats received the ferulenol 50 mg/kg intraperitoneally after 24 weeks of administration of benzo[a]pyrene and the last group, the rats were treated with ferulenol alone 50 mg/kg...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270082/%C3%AE-lactam-structured-4-4-methylsulfonyl-phenyl-1-pentyl-3-phenoxyazetidin-2-one-selectively-targets-cancerous-b-lymphocyte-mitochondria
#2
Nahal Pirahmadi, Afshin Zarghi, Ahmad Salimi, Hadi Arefi, Jalal Pourahmad
β lactam-structured Cox-2 inhibitors, possesses anti-proliferative and anti-inflammatory effects. In this research, the actions of a synthetic β lactam-structured Cox-2 inhibitor with 4-(4- (Methylsulfonyl)phenyl)-1-pentyl-3-phenoxyazetidin-2-one on cellular viability of cancerous lymphoblast obtained from patients with acute lymphocytic leukemia (ALL) and normal lymphocytes obtained from healthy donors were compared.%the cell viability of cancerouslymphoblasts and normal lymphocytes treated with β lactam derivatives were assayed with MTT test...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270081/tocilizumab-labeling-with-99mtechnetium-via-hynic-as-a-molecular-diagnostic-agent-for-multiple-myeloma
#3
Ximena Camacho, Camila Longo Machado, Maria Fernanda García, Marcelo Fernández, Natalia Oddone, Juan Benech, Juan Pablo Gambini, Hugo Cerecetto, Roger Chammas, Pablo Cabral, Eloisa Riva
BACKGROUND: Multiple myeloma (MM) incidence and mortality is increasing worldwide. Interleukin-6 (IL-6) is one of the key molecules related to growth, survival and proliferation of myeloma cells. Tocilizumab is a humanized monoclonal antibody directed against receptor of IL-6. OBJECTIVE: To radiolabel Tocilizumab with 99mTechnetium as a potential imaging agents for MM. METHODS: IL-6R expression was studied by laser confocal microscopy in MM cell lines (U266, NCI-H929 and MM1S)...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270080/current-progresses-in-metal-based-anticancer-complexes-as-mammalian-trxr-inhibitors
#4
Yizhe Cheng, Yan Qi
Reactive oxygen species (ROS) are produced as normal products of cellular metabolism, which are essential for numerous cell biological functions. Due to aberrant metabolism, oncogenic signaling activation and mitochondrial dysfunction, cancer cells generate excessive ROS that cause severe oxidative damage, finally leading to tumor cell death. Thioredoxin reductase (TrxR), as an important ROS-scavenging enzyme, is overexpressed in various human tumors and plays an important role in regulating intracellular redox homeostasis to protect cancer cells from cell death induced by substantial ROS...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270079/synthesis-and-characterization-of-water-soluble-conjugates-of-cabazitaxel-hemiesters-dextran
#5
Elahehnaz Parhizkar, Fatemeh Ahmadi, Saeid Daneshamouz, Soliman Mohammadi-Samani, Amirhossein Sakhteman, Golnaz Parhizgar
BACKGROUND: Cabazitaxel (CTX) is a second- generation taxane derivative, a class of potent anticancer drugs with very low water solubility. CTX is used in patients with resistant prostate cancer unresponsive to the first generation taxane, docetaxel. Currently marketed formulations of CTX contain high concentrations of surfactant and ethanol, which causes severe hypersensitivity reactions in patients. METHODS: In order to increase its solubility, two hemiester analogs; CTX-succinate and CTX-glutarate were synthesized and characterized...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270078/a-preliminary-study-of-the-action-of-virtosomes-from-non-dividing-cells-on-tumour-cell-replication-in-vitro-and-in-vivo
#6
Mariano Garcia-Arranz, Damian Garcia-Olmo, Luz Vega-Clemente, Maurice Stroun
BACKGROUND: A DNA-RNA-lipoprotein complex, termed a virtosome, is released spontaneously from healthy human, other mammalian, avian, amphibian and plant cells in a regulated and energy-dependent manner. Studies on human and mouse lymphocytes, hepatocytes, NIH 3T3 cells and mouse tumour cell lines have shown that virtosomes may be acting as inter-cellular messengers. In particular, virtosomes from non-dividing cells blocked 3H-thymidine incorporation into DNA in tumour cell lines. OBJECTIVE: Study of the effect of virtosomes on tumors "in vivo" and "in vitro" Methods and Results...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270077/combined-treatment-with-cci779-and-sb203580-induces-cellular-senescence-in-renal-cell-carcinoma-cell-line-via-p53-pathway
#7
Ashutosh Chauhan, Rani Ojha, Deepak Kumar Semwal, Satyendra Prasad Mishra, Ruchi Badoni Semwal
Renal cell carcinoma (RCC) is one of the most common neoplasms that occurs in the kidney and is marked by a unique biology, with a long history of poor response to conventional cancer treatments. In recent years, there have been significant advancements implemented to understanding the biology of RCC, which has led to the introduction of novel targeted therapies in the management of patients with metastatic disease. So in the present study, we evaluated the effects of p38 MAPK inhibitor (SB203580), alone and in combination with mTOR inhibitor (CCI779) on apoptosis and cell proliferation...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270076/doxycycline-as-potential-anti-cancer-agent
#8
Isra Ali, Khalid O Alfarouk, Stephan J Reshkin, Muntaser E Ibrahim
Cancer cells do create hostile microenvironment (deprivation of nutrients, accumulation of acidity, anoxic habitat). Those cells are not only adapted to this sanctuary environment, blunting of immunity but also, grow, migrate to the distal area (metastasis) and communicate with each other in a unique population structure and organization too (clonal expansion). The adaptation requirements push those types of adaptable cells (cancer cells) to be primitive cells. The prevailing pharmacological approach in treating cancer is developing a chemotherapeutic agent that acts on rapidly proliferating cells that stuck with normally growing epithelium and bone marrow too...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270075/comparative-effects-of-polo-like-kinase-1-inhibitors-as-monotherapy-and-in-combination-with-current-treatments-for-medulloblastoma
#9
Julia Alejandra Pezuk, Maria Sol Brassesco, Priscila Maria Manzini Ramos, Carlos Alberto Scrideli, Luiz Gonzaga Tone
BACKGROUND: Medulloblastoma (MB) is one of most frequent malignant tumors that affects children. Despite relative good survival rates, long time sequels are still significant and represent a challenge for treatment of MB patients. Therefore, in an attempt to reduce treatment aftereffects new therapeutic targets are constantly being explored. Polo like kinase 1 (PLK1) is a master cell cycle regulator that has been reported increased in proliferative cells, while its depletion has been repeatedly proposed as an oncological therapeutic strategy...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270074/molecular-and-thermodynamic-studies-on-dna-triplex-formed-in-the-promoter-region-of-hmgb1-gene-as-a-selective-target-for-anticancer-drugs
#10
Neelam Lohani, Rajeswari Raja Moganty
HMGB1 (High Mobility Group Box-1) is a very versatile highly abundant architectural protein that plays multiple roles in human health and diseases. Under physiological condition it serves an amazing assortment of roles in different compartments of cell. The reported high expression of HMGB1 in almost all types of human cancers and inflammatory diseases make it a critical molecular therapeutic target. In the present study we have mobilized a proximal twenty one bp nucleotide (21RY) which is in the promoter region (-55 to-75) of hmgb1 gene and targeted it with triplex forming oligonucleotide (TFO) in combination with two widely used chemotherapeutic drugs actinomycin (ACT) and adriamycin (ADM)...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270073/colon-cancer-and-specific-ways-to-deliver-drugs-to-the-large-intestine
#11
Hossein Derakhshankhah, Zhila Izadi, Alireza Lotfabadi, Loghman Alaei, Ali Akbar Saboury, Rassoul Dinarvand, Adeleh Divsalar, Arefeh Seyedarabi, Ebrahim Barzegari, Mina Evini
BACKGROUND: It has been postulated that colon cancer is the third cause of cancer death worldwide. Recently, colon-targeted drug delivery systems have been developed for improving systemic drug delivery and treatment of local colon associated diseases. Using such drug delivery systems increases the drug's effectiveness and results in reduced systemic side effects. Drug delivery systems formulated for the colon requires that the triggering of drug release mechanism is designed based on the colon's physiological conditions...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270072/topical-ingenol-mebutate-a-new-treatment-modality-for-multiple-actinic-keratoses-and-field-cancerization
#12
Kresimir Kostovic, Sandra Jerkovic Gulin, Zrinka Bukvic Mokos, Romana Ceovic
BACKGROUND: Ingenol mebutate gel is a recent stirring weapon recommended for the treatment of multiple actinic keratoses (AKs) and field cancerization. This review brings a summary of recent data on the treatment of AKs with ingenol mebutate (IM) providing critical commentary with regard to drug's characteristics, drug's safety profile, treatment regimen, treatment outcome, patient compliance, AK recurrence, cost-effectiveness and cost-utility, as well as guidelines for the management of the treatment of AK...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270071/inhibitory-effects-of-novel-sphk2-inhibitors-on-migration-of-cancer-cells
#13
Deokho Jung, Junghyun Jung, Euiyeon Lee, Chang Soo Mok, Hyunjin Jeon, Chang Seo Park, Wonhee Jang, Youngeun Kwon
Cell migration is an essential process for survival and differentiation of mammalian cells. Numerous diseases are induced or influenced by inappropriate regulation of cell migration, which plays a key role in cancer cell metastasis. In fact, very few anti-metastasis drugs are available on the market. SphKs are enzymes that convert sphingosine to sphingosine-1- phosphate (S1P) and are known to control various cellular functions, including migration of cells. Among two human isozymes of SphK2, SphK2 is known to promote apoptosis, suppresses cell growth, and controls cell migration; in addition, the specific ablation of SphK2 activity was reported to inhibit cancer cell metastasis...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270070/fine-tuning-antibody-conjugation-methods-using-snap-tag-technology
#14
Karinna Chouman, Mira Woitok, Radoslav Mladenov, Claudia Kessler, Elmar Weinhold, Gisela Hanz, Rainer Fischer, Ivo Meinhold-Heerlein, Andreas Bleilevens, Gerrit Gresch, Anka Maria Haugg, Felix Zeppernick, Dirk Bauerschlag, Nicolai Maass, Elmar Stickeler, Katharina Kolberg, Ahmad Fawzi Hussain
Background Targeted imaging and therapy (theranostics) is a promising approach for the simultaneous improvement of cancer diagnosis, prognosis and management. Therapeutic and imaging reagents are coupled to tumor-targeting molecules such as antibodies, providing a basis for truly personalized medicine. However, the development of antibody-drug conjugates with acceptable pharmaceutical properties is a complex process and several parameters must be optimized, such as the controlled conjugation method and the drug-to-antibody ratio...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270069/pathological-and-therapeutic-aspects-of-long-noncoding-rnas-in-osteosarcoma
#15
Kaixiu Wang, Wei Jiang, Chao Cheng, Yusheng Li, Min Tu
BACKGROUND: Osteosarcoma (OS) is a common bone malignant tumor, which is the eighth leading form of pediatric cancer. Despite the modern chemotherapeutic development of OS, a number of patients with OS have a high risk of lung metastasis and local relapse after chemotherapy. OBJECTIVE: This review study focused on the role of long non coding RNAs (lncRNAs) in OS progression, and presented update reports on OS treatment by targeting specific lncRNAs. METHOD: We have acquired information on OS and lncRNAs from scientific databases like google scholar, pubmed and scopus, and reviewed for this study...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270068/improving-the-hsp90-inhibitors-containing-4-2-4-dihydroxyphenyl-1-2-3-thiadiazole-scaffold-synthesis-affinity-and-effect-on-cancer-cells
#16
Egidijus Kazlauskas, Algirdas Brukštus, Herkus Petrikas, Vilma Petrikaitė, Inga Čikotienė, Daumantas Matulis
Human Hsp90 chaperone inhibitors are known to be potential anticancer drugs. A series of compounds containing the 4-(2,4-dihydroxyphenyl)-1,2,3-thiadiazole scaffold were synthesized as inhibitors of this chaperone. Their binding to the recombinant N-terminal domain of Hsp90 was determined by the fluorescence thermal shift assay, which revealed that four of these compounds bound to Hsp90 with Kd of 0.6 to 0.8 nM. The compounds fully inhibited the growth of all tested cancer cell lines: A549 (lung adenocarcinoma), IGR39 (melanoma), and U87 (glioblastoma), with the effective antiproliferative concentration (EC50) of the compounds reaching 0...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270067/the-effects-of-nanoencapsulated-curcumin-fe3o4-on-proliferation-and-htert-gene-expression-in-lung-cancer-cells
#17
Hadi Sadeghzadeh, Younes Pilehvar-Soltanahmadi, Abolfazl Akbarzadeh, Hassan Dariushnejad, Forough Sanjarian, Nosratollah Zarghami
OBJECTIVE: The aim of the study is to fabricate curcumin-loaded PLGA-PEG-Fe3O4 nanoparticles and comprise the effects of pure curcumin and curcumin-nanomagnetic encapsulated in PLGA-PEG on cell cytotoxicity and hTERT gene expression in A549 lung cancer cell line. BACKGROUND: Lung cancer is the most common cancer in men and one of the four main cancers that occurs in women. Telomerase is active in more than 85% of various cancerous cells such as lung cancer while its activity is very low in normal cells...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270066/evaluation-of-the-anticancer-activities-of-the-plant-alkaloids-sanguinarine-and-chelerythrine-in-human-breast-adenocarcinoma-cells
#18
Igor Vivian Almeida, Liliane Menezes Fernandes, Bruna Isabela Biazi, Veronica Elisa Pimenta Vicentini
BACKGROUND: Breast cancer is associated with a high mortality rate around the world due to its aggressiveness and highly resistance to conventional therapies. Sanguinarine (SAN) and Chelerythrine (CHE) are plant alkaloids extracted from Sanguinaria canadensis and Macleaya cordata, which have been studied for their bioactivities. OBJECTIVE: To determine the anticancer activities of Sanguinarine (SAN) and Chelerythrine (CHE) plant alkaloids. METHOD: It was performed the MTT assay, the alkaline comet assay and cell cycle analyses by flow cytometry...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270065/may-adjuvant-therapy-play-a-role-for-the-management-of-renal-cell-carcinoma-a-review-of-literature-and-ongoing-trials
#19
Carlo Messina, Elisa Zanardi, Francesco Boccardo
BACKGROUND: Renal cell carcinoma (RCC) is responsible for 4% of all neoplasms in adults and 80% of all primary renal tumours. In the European Union, there are almost 84000 new cases and 35000 deaths each year due to RCC. In the last five decade patients with localised RCC will develop recurrence of disease after nephrectomy in about 50% of cases. Considering the number of novel targeted therapies approved in the last years for the treatment of mRCC, there has been great interest to assess the efficacy of the same agents in the adjuvant setting...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28270064/synthesis-and-characterization-of-two-new-thiophene-acetyl-salicylic-acid-esters-and-their-ortho-and-para-effect-on-anticancer-activity
#20
Hakan Ünver, Zerrin Canturk
The present study aimed to explore the cytotoxic effect of ortho- and para-positional isomers of thiophene acetyl salicylic acid esters against cancer and normal cell lines. Two new thiophene-2-acetic acid esters (2-((2-(thiophen-2-yl)acetyl)thio)benzoic acid and 4-((2-(thiophen-2-yl)acetyl)thio)benzoic acid) were synthesized and characterized by elemental analysis, Fourier transform infrared spectroscopy, 1H-nuclear magnetic resonance (NMR), 13C-NMR, and high-resolution mass spectroscopy. The compounds were tested for their in vitro cytotoxic activity against A549 and Caco2 tumor cell lines and CCD-19Lu and CCD 841 CoN normal cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,4,diphenyltetrazolium bromide assay...
February 13, 2017: Anti-cancer Agents in Medicinal Chemistry
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