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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/29034843/research-progress-in-reversal-of-tumor-multi-drug-resistance-via-natural-products
#1
Qi Guo, Hongyan Cao, Xianghui Qi, Huikai Li, Peizhi Ye, Zhiguo Wang, Danqiao Wang, Hua Zhou, Jingui Xue, Mingyu Sun
Multidrug resistance (MDR) occurs when a tumor develops resistance to multiple chemotherapeutic drugs, which may include antitumor drugs with different chemical structures and mechanisms. MDR limits the treatment effects of antitumor drugs, and is the main cause of chemotherapy failure. MDR is caused by numerous factors including changes in ABC transporters, target proteins, detoxification, DNA repair, drug metabolic enzymes, and signal pathways of apoptosis. Clinical research indicates that natural products have great potential to treat tumors and reverse MDR...
October 16, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29034842/1-3-6-trihydroxy-7-methyl-9-10-anthracenedione-isolated-from-genus-lindera-with-anti-cancer-activity
#2
Guoqing Wei, Hui Chen, Fangyuan Nie, Xiaofeng Ma, Hezhong Jiang
Background Natural products inhibiting fatty acid synthase are potential therapeutic agents to treat cancer. Objective To investigate the chemical constituents of the root tubers of Lindera aggregate and the stems of Linderanacusua, and to find natural inhibitors on the expression level on fatty acid synthase in human breast cancer MDA-MB-231 cells. Methods The isolation and purification of the extracts were conducted by the methods of percolation and partition extraction, silica and gel column chromatography, recrystallization and by NMR and spectroscopic analysis method...
October 16, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29022515/immunopharmacological-activity-of-betulin-in-inflammation-associated-carcinogenesis
#3
Anja Schwiebs, Heinfried Radeke
This review highlights the multiple properties of the birch bark-derived pentacyclic triterpene betulin with special focus on its pharmacological activity in cancer and inflammation. While less well characterized compared to its hydrophilic derivative, betulinic acid, it exhibits potent anticancer activity described in many publications. Indeed, underinvestigated are its immunomodulatory functions in inflammatory diseases that appeared to enhance innate immune cell activities in an adjuvant-like fashion towards an interleukin-12 driven antitumor immunity...
October 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28971779/new-ferrocene-compounds-as-selective-cyclooxygenase-cox-2-inhibitors-design-synthesis-cytotoxicity-and-enzyme-inhibitory-activity
#4
Shabnam Farzaneh, Elnaz Zainalzadeh, Bahram Daraei, Soraya Shahhosseini, Afshin Zarghi
Background Due to the astonishing properties of ferrocene and its derivatives, it has a broad application in diverse areas. Numerous ferrocene derivatives demonstrated anti-proliferative activity. Also COX-2, as a key isoenzyme for production of prostaglandins, is frequently overexpressed in various cancers. It is now recognized that COX-2 over expression promotes tumorigenic functions which can be suppressed by COX-2 inhibitors, a phenomenon useful for the preventing of tumor progression. The combination of COX-2 inhibitors with other anti-cancer or cancer prevention drugs may reduce their side effects in future cancer prevention and treatment...
October 3, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28933263/anticancer-properties-of-a-new-hybrid-analog-ad-013-combining-a-coumarin-scaffold-with-an-%C3%AE-methylene-%C3%AE-lactone-motif
#5
Angelika Długosz, Katarzyna Gach-Janczak, Jacek Szymański, Dariusz Deredas, Henryk Krawczyk, Tomasz Janecki, Anna Janecka
Background Coumarin is a natural phytochemical but as such has no medical uses. However, various natural and synthetic coumarin analogs attract attention due to their interesting biological properties. </P><P> Objective Here, we evaluated and compared anticancer properties of a new synthetic hybrid compound AD-013, which integrates a coumarin moiety and an α-methylene-δ-lactone motif, with novobiocin, a natural antibiotic bearing a coumarin scaffold. </P><P> Method Cytotoxic activities of compound AD-013 and novobiocin were assessed by the MTT assay...
September 21, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28933262/the-measurement-and-mathematical-analysis-of-5-fu-release-from-magnetic-polymeric-nanocapsules-following-the-application-of-ultrasound
#6
Ziaeddin Abed, Samideh Khoei, Behafarid Ghalandari, Jaber Beik, Ali Shakeri-Zadeh, Habib Ghaznavi, Mohammad Bagher Shiran
OBJECTIVE: To study the effects of ultrasound irradiation on the release profile of 5-fluorouracil (5-Fu) loaded magnetic poly lactic co-glycolic acid (PLGA) nanocapsules. Also, the controlled drug-release behaviour of the nanocapsules was mathematically investigated. METHOD: The nanocapsules were synthesized, dispersed in phosphate buffered saline (PBS), transferred to a dialysis bag, and finally, irradiated by various ultrasound parameters (1 or 3MHz; 0.3-1W/cm2; 5-10 minutes)...
September 21, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28933271/targeting-cell-necroptosis-and-apoptosis-induced-by-shikonin-via-receptor-interacting-protein-kinases-in-estrogen-receptor-positive-breast-cancer-cell-line-mcf-7
#7
Zahra Shahsavari, Fatemeh Karami-Tehrani, Siamak Salami
Recognition of a new therapeutic agent may activate an alternative programmed cell death for the treatment of breast cancer. Here, it has been tried to evaluate the effects of Shikonin, a naphthoquinone derivative of Lithospermum erythrorhizon, on the induction of necroptosis and apoptosis mediated by RIPK1-RIPK3 in the ER+ breast cancer cell line, MCF-7. In the current study, cell death modalities, cell cycle patterns, RIPK1 and RIPK3 expressions, caspase-3 and caspase-8 activities, reactive oxygen species and mitochondrial membrane potential have been evaluated in the Shikonin-treated MCF-7 cells...
September 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28925880/antileukemic-properties-of-sesquiterpene-lactones-a-systematic-review
#8
Elaine da Silva Castro, Lívia Azeredo Alves Antunes, Jonathas Felipe Revoredo Lobo, Norman Arthur Ratcliffe, Ricardo Moreira Borges, Leandro Rocha, Patrícia Federal Burth, Lidia Maria Fonte Amorim
This review summarizes the reported molecular mechanisms underlying the antileukemic property of Sesquiterpene Lactones (SLs). This systematic review was registered in the PROSPERO database and conducted following the PRISMA Statements. The MeSH terms, Sesquiterpenes, Lactones and Leukemia were used in four databases (Pubmed, Web of Science, Scopus and Bireme). There were 281 studies selected, but after exclusions, due to replication (n = 172) or not following PECOS criteria (n = 24), 148 studies remained. Of the 148 articles, only 22 were submitted to quality assessment and were scored in high level if more than two techniques, to elucidate antileukemic proprieties, were described, and then data were extracted...
September 18, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28925879/human-fibronectin-extra-domain-b-edb-speci%C3%AF-c-aptide-aptedb-radiolabelling-with-technetium-99m-as-a-potent-targeted-tumour-imaging-agent
#9
Mohsen Mohammadgholi, Nourollah Sadeghzadeh, Mostafa Erfani, Saeid Abediankenari, Seyed Mohammad Abedi, Iman Emrarian, Narjes Jafari, Ramezan Behzadi
BACKGROUND: Human fibronectin extra-domain B (EDB) is particularly expressed during angiogenesis progression. It is, thus, a promising marker of tumour growth. Aptides are a novel class of peptides with high-affinity binding to specific protein targets. APTEDB is an antagonist-like ligand that especially interacts with human fibronectin EDB. OBJECTIVE: This study was the first attempt in which the hydrazinonicotinamide (HYNIC)-conjugated APTEDB was labelled with technetium-99m (99mTc) as an appropriate radiotracer and tricine/EDDA exchange labeling ...
September 18, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28925878/genistein-induces-alterations-of-epigenetic-modulatory-signatures-in-human-cervical-cancer-cells
#10
Madhumitha Kedhari Sundaram, Mohammad Zeeshan Ansari, Abdullah Al Mutery, Maryam Ashraf, Reem Nasab, Sheethal Rai, Naushad Rais, Arif Hussain
Introduction Epidemiological studies indicate that diet rich in fruits and vegetables are associated with decreased cancer risk thereby indicating that dietary polyphenols can be potential chemo-preventive agents. The reversible nature of epigenetic modifications makes them a favorable target for cancer prevention. Polyphenols have been shown to reverse aberrant epigenetic patterns by targeting the regulatory enzymes, DNA methyltransferases (DNMTs) and histone deacetylases (HDACs). In vitro and in silico studies of DNMTs and HDACs were planned to examine genistein's role as a natural epigenetic modifier in human cervical cancer cells, HeLa...
September 18, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28925877/4-aryl-heteroaryl-4h-fused-pyrans-as-anti-proliferative-agents-design-synthesis-and-biological-evaluation
#11
Dinesh Kumar, Gurpreet Singh, Pooja Sharma, Arem Qayum, Girish Mahajan, M J Mintoo, Shashank Kumar Singh, Dilip Manikrao Mondhe, Pms Bedi, Subheet K Jain, Girish Kumar Gupta
The current study is focused on the design and synthesis of 4-aryl/heteroaryl-4H-fused pyrans as anti-proliferative agents. All the synthesized molecules were screened against a panel of human carcinoma cell lines. Significant inhibition was exhibited by the compounds against HCT-116 (Colon) and PC-3 (Prostate) cell lines while A-549 (Lung) cell lines, MiaPaCa-2 (Pancreatic) cell lines and HL-60 (Leukemia Cancer) cell lines were almost resistant to the exposure of the test compounds. Compound FP-(v)n displayed noteworthy cytotoxicity towards HCT-116 malignant cells with IC50 value of 0...
September 18, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28925876/the-antitumor-potential-of-marine-natural-products-a-mechanistic-investigation
#12
Liping Hu, Jie Ying, Miaomiao Zhang, Xiaoyan Qiu, Yu Lu
Compounds obtained from natural resources have been the important candidates for the discovery and development of drugs. Over the past few decades, marine resources gradually attracted the attention of the majority of researchers, and a number of compounds with various structures or activities have been obtained from sponge, alga, fungus, mollusks and some others. Because of the living conditions in the ocean are higher pressures, more variable temperatures, lower oxygen and lower light than that in the terrestrial environment, marine resources have a lot of organisms that are not available or rare on land...
September 18, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901264/inhibition-of-proliferation-and-induction-of-apoptosis-by-thymoquinone-via-modulation-of-tgf-family-p53-p21-and-bcl-2%C3%AE-in-leukemic-cells
#13
Mona Diab Assaf, Josiane Semaan, Marwan El-Sabban, Soad K Al-Jaouni, Rania Azar, Mohammad Amjad Kamal, Steve Harakeh
The rationale of the current study was to investigate whether the inverse association between vitamin D deficiency and parathyroid hormone levels is age-dependent and whether it has any role in modulating renal function and insulin resistance. To test this hypothesis, we have carried out a hospital based study enrolling 848 subjects (558 men and 290 women) with the mean age of 50.9±15.9 y. Vitamin D deficiency was predominant irrespective of age group (p=0.21) and gender (p=0.12). An inverse association between vitamin D and PTH was observed (r= -0...
September 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901263/%C3%AE-aroylketene-dithioacetal-mediated-synthesis-of-e-3-benzo-d-thiazol-2-ylamino-2-1-methyl-1h-indole-3-carbonyl-3-methylthio-acrylonitrile-derivatives-and-their-biological-evaluation
#14
Pravin Bhale, Hemant Vilas Chavan, Sakharam B Dongare, Sagar T Sankpal, Babasaheb P Bandgar
• Background: The blending of two pharmacophores would generate novel molecular templates that are likely to exhibit interesting biological properties. • Objective: A facile, efficient and high yielding synthesis of (E)-3-(benzo[d]thiazol-2-ylamino)-2-(1-methyl-1H-indole-3-carbonyl)-3-(methylthio) acrylonitrile derivatives and evaluation of therapeutic potential. • Method: The synthesis of target molecules has been achieved by reacting 2-aminobenzothiazole and substituted 2-(1-methyl-1H-indole-3-carbonyl)-3,3-bis(methylthio)acrylonitrile in the presence of a catalytic amount of sodium hydride in THF...
September 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901262/novel-findings-of-anti-cancer-property-of-propofol
#15
Jiaqiang Wang, Chien-Shan Cheng, Yan Lu, Xiaowei Ding, Minmin Zhu, Changhong Miao, Jiawei Chen
Propofol, a widely used intravenous anesthetic agent, is traditionally applied for sedation and general anesthesia. Recent attention has been drawn to explore the role and mechanisms of Propofol against cancer progression in vitro and in vivo. Specifically, the proliferation-inhibiting and apoptosis-inducing properties of Propofol in cancer have been studied. However, the underlying mechanisms remain unclear. This review focuses on research advancements of the recent ten years and aims to provide a general overview of Propofol's malignance-modulating properties and the underlying molecular mechanisms...
September 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901261/spices-with-breast-cancer-chemopreventive-and-therapeutic-potentials-a-functional-foods-based-review
#16
Aliyu Muhammad, Mohammed Auwal Ibrahim, Ochuko Lucky Erukainure, Ibrahim Malami, Auwal Adamu
Cancer is a disease that affects a significant number of both rural and urban dwellers. Among the various types of cancer, breast cancer is one of the most common diagnosed cancers among females. Its menace can be curbed with locally consumed spices due to their multiple bioactive phytochemicals. This review focuses on the breast cancer chemopreventive and therapeutic potentials of locally consumed spices. The most commonly consumed spices with breast cancer chemopreventive and chemotherapeutic phytochemical include pepper, onions, ginger, garlic, curry and thyme containing many biologically active metabolites ranging from vitamins, fatty acids esters, polyphenols/phenolics, sulfur-containing compounds and anthraquinones with proven antioxidant, anti-inflammatory, immuno-modulatory, antitumor and anticancer properties against breast cancer/carcinogenesis...
September 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901258/from-biology-to-therapy-improvements-of-therapeutic-options-in-lung-cancer
#17
Luigi Formisano, Valerie M Jansen, Roberta Marciano, Roberto Bianco
Lung cancer is the leading cause of cancer-related mortality around the world, despite effective chemotherapeutic agents, the prognosis has remained poor for a long time. The discovery of molecular changes that drive lung cancer has led to a dramatic shift in the therapeutic landscape of this disease. In "in vitro" and "in vivo" models of NSCLC (non-small cell lung cancer), angiogenesis blockade has demonstrated an excellent anti-tumor activity, thus, a number of anti-angiogenic drugs have been approved by regulatory authorities for use in clinical practice...
September 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901257/molecular-characterization-of-two-polysaccharides-from-phellinus-vaninii-ljup-and-their-anti-tumor-activities
#18
Xuewei Jia, Mingqi Gao, Mingzhe Li, Ying Zheng, Chun-Ping Xu
Two water-soluble polysaccharides (PV-W, PV-B) were isolated and purified from fruiting bodies of P. vaninii Ljup (a traditional Chinese medicine) by hot water and sodium hydroxide, respectively. The chemical structure was analyzed by FT-IR, GC-MS analysis and 13C NMR spectra. The results illustrated that PV-W was a heteropolysaccharide, mainly composed of mannose, glucose, arabinose and galactose. PV-B was a β-1, 3-D-glucan branched with β-1, 6-D-glucose. The results of viscometry proved that PV-W and PV-B could be molecularly dispersed in water without aggregation...
September 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901265/stereocomplexation-assisted-assembly-of-poly-g-glutamic-acid-graft-polylactide-nano-micelles-and-their-efficacy-as-anticancer-drug-carrier
#19
Shulin Dai, Yucheng Feng, Shuyi Li, Yuxiao Chen, Meiqing Liu, Chao Zhang, Wei Zhang, Yihua Yin
Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. In this paper, stereocomplexed micelles (γ-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(γ-glutamic acid)-graft-PLLA (γ-PGA-g-PLLA) and poly(γ-glutamic acid)-graft-PDLA (γ-PGA-g-PDLA)...
September 11, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28901260/vdac1-mediated-anticancer-activity-of-gallic-acid-in-human-lung-adenocarcinoma-a549-cells
#20
Aikebaier Maimaiti, Amier Aili, Hureshitanmu Kuerban, Xuejun Li
Gallic acid (GA) is generally distributed in a variety of plants and foods, and possesses cell growth-inhibiting activities in cancer cell lines. In the present study, the impact of GA on cell viability, apoptosis induction and possible molecular mechanisms in cultured A549 lung carcinoma cells was investigated. In vitro experiments showed that treating A549 cells with various concentrations of GA inhibited cell viability and induced apoptosis in a dose-dependent manner. In order to understand the mechanism by which GA inhibits cell viability, comparative proteomic analysis was applied...
September 11, 2017: Anti-cancer Agents in Medicinal Chemistry
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