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https://www.readbyqxmd.com/read/28635648/deoxyelephantopin-and-isodeoxyelephantopin-as-potential-anticancer-agents-with-effects-on-multiple-signaling-pathways
#1
REVIEW
Tahir Mehmood, Amara Maryam, Hamed A Ghramh, Muhammad Khan, Tonghui Ma
Cancer is the 2nd leading cause of death worldwide. The development of drugs to target only one specific signaling pathway has limited therapeutic success. Developing chemotherapeutics to target multiple signaling pathways has emerged as a new prototype for cancer treatment. Deoxyelephantopin (DET) and isodeoxyelephantopin (IDET) are sesquiterpene lactone components of "Elephantopus scaber and Elephantopus carolinianus", traditional Chinese medicinal herbs that have long been used as folk medicines to treat liver diseases, diabetes, diuresis, bronchitis, fever, diarrhea, dysentery, cancer, and inflammation...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28629630/design-synthesis-and-tumor-cell-growth-inhibitory-activity-of-3-nitro-2h-cheromene-derivatives-as-histone-deacetylaes-inhibitors
#2
Shuai Tan, Feng He, Tingting Kong, Jingde Wu, Zhaopeng Liu
As a continuous research for the discovery of coumarin-based targeted anticancer agents, we designed and synthesized a series of novel histone deacetylases (HDAC) inhibitors using the 8-ethoxy-3-nitro-2H-chromene as the surface binding or cap group, linear dicarboxylic acid or ω-amino acid moiety with different length as the linking motif, ortho-aminoanilides, amides or α-aminoamides as the zinc binding group and the internal cavity motifs. Most of these 3-nitro-2H-chromene derivatives exhibited good growth inhibitory activity against K562, A549, MCF-7, PC3 and Hela cells and were more potent than the reference drug SAHA and MS-275...
June 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28629184/determination-of-structural-requirements-of-n-substituted-tetrahydro-%C3%AE-carboline-imidazolium-salt-derivatives-using-in-silico-approaches-for-designing-mek-1-inhibitors
#3
Jingwei Liang, Mingyang Wang, Xinyang Li, Xin He, Chong Cao, Fanhao Meng
Novel N-substituted tetrahydro-β-carboline imidazolium salt derivatives proved to have potent antitumor activity in past research. The Topomer CoMFA and CoMSIA function in Sybyl-X 2.0 software was applied for the identification of important features of N-substituted tetrahydro-β-carboline-imidazolium salt derivative moieties. In the case of Topomer CoMFA, all the compounds were split into two fragments which were used to generate a 3D invariant representation, the statistical results of the Topomer CoMFA model: q² value of 0...
June 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28629133/propolis-diterpenes-as-a-remarkable-bio-source-for-drug-discovery-development-a-review
#4
REVIEW
Noushin Aminimoghadamfarouj, Alireza Nematollahi
Propolis is one of the complex, but valuable, bio-sources for discovering therapeutic compounds. Diterpenes are organic compounds composed of four isoprene units and are known for their biological and pharmacological characteristics, such as antibacterial, anticancer, and anti-inflammatory activities. Recently, advancements have been made in the development of antibacterial and anticancer leads from propolis-isolated diterpenes, and scrutiny of these compounds is being pursued. Thus, this review covers the progress in this arena, with a focus on the chemistry and biological activities of propolis diterpenes...
June 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28629035/sodium-alginate-polyvinyl-alcohol-bovin-serum-albumin-coated-fe3o4-nanoparticles-as-anticancer-drug-delivery-vehicle-doxorubicin-loading-and-in-vitro-release-study-and-cytotoxicity-to-hepg2-and-l02-cells
#5
G Prabha, V Raj
The challenging part of this work was to research the potential aspects of sodium alginate (SA)-polyvinyl alcohol (PVA)-bovin serum albumin (BSA) coated Fe3O4 nanoparticles (Fe3O4-SA-PVA-BSA) as a drug delivery system for doxorubicin (DOX). The anticancer drug doxorubicin was selected as a model drug which is powerful for numerous cancer treatments. Superparamagnetic Fe3O4 nanoparticles were prepared by co-precipitation method. The mixture solution of Fe3O4-sodium alginate (SA) - doxorubicin (DOX) was crosslinked with Ca(2+) to form (Fe3O4-SA-DOX) nanoparticles and addition of PVA and BSA with (Fe3O4-SA-DOX) nanoparticles was prepared by coating procedure...
October 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28626426/potential-of-central-eastern-and-western-africa-medicinal-plants-for-cancer-therapy-spotlight-on-resistant-cells-and-molecular-targets
#6
REVIEW
Armelle T Mbaveng, Victor Kuete, Thomas Efferth
Cancer remains a major health hurdle worldwide and has moved from the third leading cause of death in the year 1990 to second place after cardiovascular disease since 2013. Chemotherapy is one of the most widely used treatment modes; however, its efficiency is limited due to the resistance of cancer cells to cytotoxic agents. The present overview deals with the potential of the flora of Central, Eastern and Western African (CEWA) regions as resource for anticancer drug discovery. It also reviews the molecular targets of phytochemicals of these plants such as ABC transporters, namely P-glycoprotein (P-gp), multi drug-resistance-related proteins (MRPs), breast cancer resistance protein (BCRP, ABCG2) as well as the epidermal growth factor receptor (EGFR/ErbB-1/HER1), human tumor suppressor protein p53, caspases, mitochondria, angiogenesis, and components of MAP kinase signaling pathways...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28621561/a-patent-review-of-two-fruitful-decades-1997-2016-of-isocoumarin-research
#7
Hidayat Hussain, Ivan R Green
Isocoumarins comprise a six-membered oxygen heterocycle (α-pyranone) along with one aromatic ring and are known to possess interesting biological properties. During the last two decade (1997-2016), isocoumarin chemistry has attracted attention due to its biological and pharmaceutical effects viz., anticancer, anti-diabetic, antibacterial, antimalarial, and fungicidal effects. Areas covered: This review covers the patents on the therapeutic activities of natural and synthetic isocoumarins over the last two decades (1997-2016)...
June 16, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28621163/eribulin-in-advanced-liposarcoma-and-leiomyosarcoma
#8
Elisabetta Setola, Jonathan Noujaim, Charlotte Benson, Sant Chawla, Emanuela Palmerini, Robin L Jones
The heterogeneity of soft tissue sarcomas (STS) presents a formidable management challenge. Consequently, one of the main research goals is to define specific tailored therapy for each histological subtype and to develop a more personalised approach to treatment. The standard first line chemotherapy for advanced STS is doxorubicin, with or without ifosfamide, however, a number of different drugs are emerging as active therapies beyond first-line. Areas covered: Eribulin has recently been approved for advanced liposarcoma, after an anthracycline-containing regimen, demonstrating an overall survival (OS) advantage in liposarcoma and leiomyosarcoma in a randomised Phase III clinical trial...
June 16, 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/28621113/alteration-of-dna-methylation-in-gastric-cancer-with-chemotherapy
#9
REVIEW
Su Jin Choi, Seok Won Jung, Sora Huh, Yoon-Seok Chung, Hyosun Cho, Hyojeung Kang
Epigenetic alterations such as DNA methylation, histone acetylation, and chromatin remodeling can control gene expression by regulating gene transcription. DNA methylation is one of the frequent epigenetic events that play important roles in cancer development. Cancer cells can gain significant resistance to anticancer drugs and escape programmed cell death through major epigenetic changes, including DNA methylation. To date, several research groups have identified instances of both 1) hypermethylation of tumor suppressor genes, and 2) global hypomethylation of oncogenes...
June 16, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28618001/three-dimensional-cell-culture-models-for-anticancer-drug-screening-worth-the-effort
#10
REVIEW
Eddy-Tim Verjans, Jordi Doijen, Walter Luyten, Bart Landuyt, Liliane Schoofs
High attrition of new oncology drug candidates in clinical trials is partially caused by the poor predictive capacity of artificial monolayer cell culture assays early in drug discovery. Monolayer assays do not take the natural three-dimensional (3D) microenvironment of cells into account. As a result, false positive compounds often enter clinical trials, leading to high dropout rates and a waste of time and money. Over the past two decades, tissue engineers and cell biologists have developed a broad range of 3D in vitro culturing tools that better represent in vivo cell biology...
June 15, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28615941/development-and-optimization-of-an-injectable-formulation-of-copper-diethyldithiocarbamate-an-active-anticancer-agent
#11
Mohamed Wehbe, Malathi Anantha, Minghan Shi, Ada Wai-Yin Leung, Wieslawa H Dragowska, Léon Sanche, Marcel B Bally
Copper diethyldithiocarbamate (Cu(DDC)2) is the active anticancer agent generated when disulfiram (DSF) is provided in the presence of copper. To date, research directed toward repurposing DSF as an anticancer drug has focused on administration of DSF and copper in combination, efforts that have proven unsuccessful in clinical trials. This is likely due to the inability to form Cu(DDC)2 at relevant concentrations in regions of tumor growth. Little effort has been directed toward the development of Cu(DDC)2 because of the inherent aqueous insolubility of the complex...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28615519/the-reverse-warburg-effect-is-likely-to-be-an-achilles-heel-of-cancer-that-can-be-exploited-for-cancer-therapy
#12
REVIEW
Yaojie Fu, Shanshan Liu, Shanghelin Yin, Weihong Niu, Wei Xiong, Ming Tan, Guiyuan Li, Ming Zhou
Although survival outcomes of cancer patients have been improved dramatically via conventional chemotherapy and targeted therapy over the last decades, there are still some tough clinical challenges that badly needs to be overcome, such as anticancer drug resistance, inevitable recurrences, cancer progression and metastasis. Simultaneously, accumulated evidence demonstrates that aberrant glucose metabolism termed 'the Warburg effect' in cancer cell is closely associated with malignant phenotypes. In 2009, a novel 'two-compartment metabolic coupling' model, also named 'the reverse Warburg effect', was proposed and attracted lots of attention...
May 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28609434/pharmacologically-directed-strategies-in-academic-anticancer-drug-discovery-based-on-the-european-nci-compounds-initiative
#13
Hans R Hendriks, Anne-Sophie Govaerts, Iduna Fichtner, Sally Burtles, Andrew D Westwell, Godefridus J Peters
BACKGROUND: The European NCI compounds programme, a joint initiative of the EORTC Research Branch, Cancer Research Campaign and the US National Cancer Institute, was initiated in 1993. The objective was to help the NCI in reducing the backlog of in vivo testing of potential anticancer compounds, synthesised in Europe that emerged from the NCI in vitro 60-cell screen. METHODS: Over a period of more than twenty years the EORTC-Cancer Research Campaign panel reviewed ∼2000 compounds of which 95 were selected for further evaluation...
June 13, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28606050/insights-into-the-targeting-potential-of-thymoquinone-for-therapeutic-intervention-against-triple-negative-breast-cancer
#14
Md Abul Barkat, Harshita Abul, Javed Ahmad, Mohammad Ahmed Khan, Sarwar Beg, Farhan Jalees Ahmad
BACKGROUND: Thymoquinone (TQ) is a bioactive phytoconstituent obtained from Nigella sativa (black seeds). It has promising potential in cancer prevention. OBJECTIVE: Previous studies have shown that TQ can modulate signaling pathways responsible for cancer progression, thus enhances the efficacy and improve safety profile of clinically used anticancer drugs. METHOD: TQ acts on cell cycle and inhibits progression from G1 to S phase by targeting various proteins (cyclin D1, cyclin E, and p27)...
June 11, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28604114/an-omics-perspective-to-the-molecular-mechanisms-of-anticancer-metallo-drugs-in-the-computational-microscope-era
#15
Angelo Spinello, Alessandra Magistrato
Introduction Metallo-drugs have attracted enormous interest for cancer treatment. The achievements of this drug-type are summarized by the success story of cisplatin. That being said, there have been many drawbacks with its clinical use, which prompted decades worth of research efforts to move towards safer and more effective agents, either containing platinum or different metals. Areas Covered In this review, the authors provide an atomistic picture of the molecular mechanisms involving selected metallo-drugs from structural and molecular simulation studies...
June 12, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28600785/clinical-development-of-anti-mitotic-drugs-in-cancer
#16
Anna-Maria Olziersky, S Intidhar Labidi-Galy
Mitosis is one of the most fundamental processes of life by which a mammalian cell divides into two daughter cells. Mitosis has been an attractive target for anticancer therapies since fast proliferation was identified as one of the hallmarks of cancer cells. Despite efforts into developing specific inhibitors for mitotic kinases and kinesins, very few drugs have shown the efficiency of microtubule targeting-agents in cancer cells with paclitaxel being the most successful. A deeper translational research accompanying clinical trials of anti-mitotic drugs will help in identifying potent biomarkers predictive for response...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28600665/determination-of-degradation-kinetics-and-effect-of-anion-exchange-resin-on-dissolution-of-novel-anticancer-drug-rigosertib-in-acidic-conditions
#17
Hardikkumar H Patel, Manoj Maniar, Chen Ren, Rutesh H Dave
Rigosertib is a novel anticancer drug in clinical development by Onconova therapeutics, Inc. Currently, it is in pivotal phase III clinical trials for myelodysplastic syndrome (MDS) patients. Chemically, it is a sodium salt of weak acid with low solubility in lower pH solutions. In the preliminary studies, it was found that rigosertib is unstable in acidic conditions and forms multiple degradation products. In this research, drug degradation kinetics of rigosertib were studied in acidic conditions. Rigosertib follows pseudo-first-order general acid catalysis reaction...
June 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28595492/current-mathematical-models-for-cancer-drug-discovery
#18
Letizia Carrara, Silvia Maria Lavezzi, Elisa Borella, Giuseppe De Nicolao, Paolo Magni, Italo Poggesi
Pharmacometric models represent the most comprehensive approache for extracting, summarizing and integrating information obtained in the often sparse, limited, and less-than-optimally designed experiments performed in the early phases of oncology drug discovery. Whilst empirical methodologies may be enough for screening and ranking candidate drugs, modeling approaches are needed for optimizing and making economically viable the learn-confirm cycles within an oncology research program and anticipating the dose regimens to be investigated in the subsequent clinical development...
June 8, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28581009/decoding-the-anticancer-activity-of-vo-clioquinol-compound-the-mechanism-of-action-and-cell-death-pathways-in-human-osteosarcoma-cells
#19
Ignacio E León, Paula Díez, Enrique J Baran, Susana B Etcheverry, Manuel Fuentes
Vanadium compounds were studied in recent years by considering them as a representative of a new class of non-platinum metal anticancer drugs. However, a few challenges still remain in the discovery of new molecular targets of these new metallodrugs. Studies on cell signaling pathways related to vanadium compounds have scarcely been reported and so far this information is highly critical for identifying novel targets that play a key role in the antitumor actions of vanadium complexes. This research deals with the alterations in the intracellular signaling pathways promoted by an oxovanadium(iv) complex with the clioquinol (5-chloro-7-iodo-8-quinolinol), VO(CQ)2, on a human osteosarcoma cell line (MG-63)...
June 5, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/28579004/sirna-delivery-system-based-on-magnetic-nanovectors-characterization-and-stability-evaluation
#20
Mohammed Abdelrahman, Laurence Douziech Eyrolles, Suad Y Alkarib, Katel Hervé-Aubert, Sanaa Ben Djemaa, Hervé Marchais, Igor Chourpa, Stephanie David
Gene therapy and particularly small interfering RNA (siRNA) is a promising therapeutic method for treatment of various human diseases, especially cancer. However the lack of an ideal delivery system limits its clinical applications. Effective anticancer drug development represents the key for translation of research advances into medicines. Previously we reported, the optimization of magnetic siRNA nanovectors (MSN) formulation based on superparamagnetic iron oxide nanoparticles (SPION) and chitosan for systemic administration...
June 1, 2017: European Journal of Pharmaceutical Sciences
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