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    1468 results match your criteria Anti-Cancer Agents in Medicinal Chemistry[Journal]

    1 OF 30

    Radio-Modulatory Potential ofCaffeic Acid Phenethyl Ester: A Therapeutic Perspective.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Radiation and Cancer Therapeutics Lab, School of Life Sciences, Jawaharlal Nehru University, New Delhi 110067. India.
    Use of natural agents is an upcoming area of research in cancer biology. Caffeic acid phenethyl ester has received great attention because of its therapeutic potential in various conditions including cancer. It is an active/abundant component of propolis. Read More

    A review on the management of small renal masses: active surveillance versus surgery.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Department of Urology, San Giovanni Battista Hospital, Citta della Salute e della Scienza, University of Turin, Turin. Italy.
    Despite the rise of small renal tumour (SRMs) diagnosis and related surgeries, death rate of kidney cancer is increasing, suggesting a non-optimal management of SRMs. Active Surveillance (AS) for kidney cancer was introduced to face this paradox. However, incertitude remains on whether and when AS can replace surgery in selected patients. Read More

    Ganoderma lucidum Polysaccharides as An Anti-cancer Agent.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Louisiana State University Health Sciences Center, Shreveport, LA. United States.
    The mushroom Ganoderma lucidum (G. lucidum) has been used for centuries in Asian countries to treat various diseases and to promote health and longevity. Clinical studies have shown beneficial effects of G. Read More

    A review of electroporation-based antitumor skin therapies and investigation of betulinic acid-loaded ointment.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Department of Pharmaceutical Technology - University of Szeged, Szeged, H-6720. Hungary.
    Background: Electrochemotherapy is a novel treatment for cutaneous and subcutaneous tumors utilizing the combination of electroporation and chemotherapeutic agents. Since tumors have an increasing incidence nowadays as a result of environmental and genetic factors, electrochemotherapy could be a promising treatment for cancer patients.

    Objective: The aim of this article is to summarize the novel knowledge about the use of electroporation for antitumor treatments and to present a new application of electrochemotherapy with a well-known plant derived antitumor drug betulinic acid. Read More

    Steroidal anticancer agents: an overview of estradiol-related compounds.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Faculty of Pharmacy, University of Szeged, Szeged, Hungary - Department of Pharmacodynamics and Biopharmacy Szeged. Hungary.
    Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc. Read More

    Growth kinetics and oncologic outcomes for small renal masses managed with active surveillance: a review of the literature.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Division of Urology, Department of Surgery, MD Anderson Cancer Center at Cooper, Cooper Medical School of Rowan University, Camden, NJ. United States.
    An increasing number of enhancing renal masses are being discovered incidentally on cross-sectional imaging. Many can be characterized as small renal masses (SRMs), the natural history of which is heterogeneous and poorly understood. Active surveillance has been proposed as an initial management strategy for these tumors, particularly in the old and infirmed patient population. Read More

    New Histopathological & Genetic Features to Improve Active Surveillance Selection for Low-Risk Prostate Cancer.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    TissuPath Specialist Pathology, Melbourne. Australia.
    Background: A recent surge in biomarkers to aid management of men with prostate cancer has occurred. Their applications are varied and not all tests are applicable to the active surveillance setting.

    Objective: To review primary evidence on genetic and immunohistochemical biomarkers, and their role on patient selection and risk stratification for men on active surveillance for prostate cancer. Read More

    Modulation of Cancer Metabolism by Phytochemicals - A Brief Overview.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    "Victor Babes" University of Medicine and Pharmacy, Timisoara - Department of Functional Sciences - Pathophysiology Timisoara. Romania.
    Despite tremendous research efforts for effective therapies, cancer remains the plague of the century and its burden is expected to increase worldwide in the near future. Metabolic reprogramming is a firmly established hallmark of all cancers, regardless their cellular or tissue origin, being a prerequisite for both tumor growth and invasion. Functional dependence of tumors on glycolysis and glutaminolysis and the crucial contribution of mitochondria to the tumor bioenergetic versatility are well recognized features and established therapeutic targets. Read More

    Halilectin-3, a lectin from the marine sponge Haliclona caerulea, induces apoptosis and autophagy in human breast cancer MCF7 cells through caspase-9 pathway and LC3-II protein expression
    Anticancer Agents Med Chem 2017 11 13. Epub 2017 Nov 13.
    UCIBIO, Departamento de Ciências da Vida, Faculdade de Ciências e Tecnologia, Universidade NOVA de Lisboa, 2829-516, Caparica, Portugal
    Background: An ideal strategy for cancer treatment is the specific induction of tumor cell death, sparing normal cells. Marine sponges are rich biological reservoirs of biomolecules, especially lectins, which have attracted considerable attention due to potential biological effect on human cells. Lectins are proteins that bind specific carbohydrate signatures and some gained further interest for their capacity to bind tumor associated carbohydrates antigens and induce tumor cell apoptosis. Read More

    Selecting Patients With Small Renal Masses For Active Surveillance.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    The James Buchanan Brady Urological Institute and Department of Urology Johns Hopkins Hospital, Baltimore, Maryland. United States.
    The incidentally discovered, clinically-localized, small renal mass (clinical stage T1aN0M0, ≤4cm) is the most commonly diagnosed entity in renal cell carcinoma (RCC) - now accounting for at least 40% of newly diagnosed renal tumors. Given the above argument, active surveillance (AS) has emerged as a viable management strategy for SRM. This review will examine and discuss the existing literature regarding selection criteria for AS. Read More

    Evaluation of antineoplastic effects of NF-κB inhibition by DHMEQ (Dehydroxymethylepoxyquinomicin) in medulloblastoma cell lines.
    Anticancer Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.
    Ribeirao Preto Medical School, University of Sao Paulo - Department of Pediatrics and Deparment of Genetics Ribeirao Preto. Brazil.
    Purpose: NF-κB is a transcription factor involved in the transcriptional regulation of a large number of genes related to tumorigenesis in several cancer cell types, and it's inhibition have been related to anticancer effect. DHMEQ (Dehydroxymethylepoxyquinomicin) is a compound that blocks the translocation of NF-κB from the cytoplasm to the nucleus, thus inhibiting its activity as a transcriptional activator. Several studies have shown the antineoplastic effects of DHMEQ in numerous tumor types, however, there are no surveys that tested their effects in MB. Read More

    Synthesis of Biotinylated 2-Methoxystrypandrone and Identification of JAK2 and IKK as its Targets.
    Anticancer Agents Med Chem 2017 Nov 6. Epub 2017 Nov 6.
    Shanghai Institute of Materia Medica. China.
    Background: 2-Methoxystypandrone (2-MS), isolated from the roots of Polygonum cuspidatum, is a potent dual inhibitor of STAT3 and NF-κB pathways.

    Objective: To investigate the molecular targets and mechanisms of 2-MS.

    Method: A biotin-conjugated 2-MS analog, named 2-MS-Biotin, was designed and synthesized. Read More

    The Impact of Translational Research in Breast Cancer Care: Can We Improve the Therapeutic Scenario?
    Anticancer Agents Med Chem 2017 Nov 2. Epub 2017 Nov 2.
    Baylor College of Medicine, Houston. - Medical Oncology Houston. United States.
    Traditionally, breast cancer (BC) is divided into different immunohistochemically (IHC)-defined subtypes, according to the expression of hormone receptors and overexpression/amplification of human epidermal growth factor receptor 2 (HER2), with crucial therapeutic implications. In the last few years, the definition of different BC molecular subgroups within the IHC-defined subtypes and the identification of the important role that molecular heterogeneity can play in tumor progression and treatment resistance have inspired the search for personalized therapeutic approaches. In this scenario, translational research represents a key strategy to apply knowledge from cancer biology to the clinical setting, through the study of all the tumors "omics", including genomics, transcriptomics, proteomics, epigenomics, and metabolomics. Read More

    The Rationale for Repurposing Sildenafil as an Adjuvant to Lung Cancer Treatment.
    Anticancer Agents Med Chem 2017 Nov 2. Epub 2017 Nov 2.
    Department of Pharmacology & Toxicology, Otago School of Biomedical Sciences, University of Otago, Dunedin. New Zealand.
    There is now a considerable body of evidence for sildenafil possessing anticancer properties. In this article we argue the case for testing sildenafil as a lung cancer therapy chemoadjuvant. Currently, lung cancer is a disease with insufficient treatment options, with only 20% of patients responding to systemic chemotherapy, and even incremental potential improvements should be explored. Read More

    Combined Evaluation of Expression of Cxcr4 and Nrf2 as Prognostic Factor for Patients with Gastric Carcinoma.
    Anticancer Agents Med Chem 2017 Nov 3. Epub 2017 Nov 3.
    The First Affiliated Hospital of Xi'an Jiaotong University - Department of Respiratory and Critical Care Medicine Xi'an, Shaanxi. China.
    CXC Chemokine Receptor 4 (CXCR4) and NFE-related factor 2 (Nrf2) have been observed implicated with cell malignant behavior of human cancers. In this study we detected their expression in gastric carcinoma (GC) tissue specimens and related the result with clinicopathological data and patient survival. 120 GC and corresponding distant normal tissue specimens were processed for immunohistochemical and qRT-PCR to analyses the expression of CXCR4 and Nrf2. Read More

    Recent Advancements in Organotin(IV) Complexes as Potential Anticancer Agents.
    Anticancer Agents Med Chem 2017 Nov 6. Epub 2017 Nov 6.
    Guru Jambheshwar University of Science and Technology Hisar. India.
    Cancer is a multistep disease incorporating physical, chemical, environmental, metabolic and genetic factors, which play direct or indirect role in the induction and deterioration of cancer. Many of the platinum based drugs were synthesized but due to their systemic toxicity, broad spectrum of action, intrinsic and acquired drug resistivity, it has become necessary to search for the effective anticancer drugs with superior efficiency. Among non-platinum metal compounds with antitumor activity, organotin complexes have proven effective management of toxicity, specific targeted drug uptake by the cancerous cell line and significant potential in the pharmaceutical chemistry. Read More

    A review of the components of seaweeds as potential candidates in cancer therapy.
    Anticancer Agents Med Chem 2017 Nov 6. Epub 2017 Nov 6.
    Hefei University of Technology - School of Medical Engineering Hefei, ChinaSchool of Medical Engineering, Hefei University of Technology, Hefei 230009, P.R. China HeFei. China.
    The marine natural products (MNPs) isolated from seaweeds-associated microbial communities have been caused a substantial part of attention owing to their exceptional nutritional and pharmacology application, such as antiviral, anticancer, antiprotozoal, antifungal, and antibacterial properties and so on. Particularly, there are several MNPs have been displayed attractive value for developing novel anticancer agents for clinical application. This review covers the literature published in the recent 5 years for the isolation and identification of novel anticancer MNPs from seaweeds. Read More

    Recent Development of Sulfonyl or Sulfonamide Hybrids as Potential Anticancer Agents: A Key Review.
    Anticancer Agents Med Chem 2017 Nov 3. Epub 2017 Nov 3.
    Wuhan University of Technology - Department of Pharmaceutical Engineering and School of Chemistry Wuhan, Hubie. China.
    Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, large numbers of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Read More

    CJK-7, a novel flavonoid from Paulownia tomentosa, triggers cell death cascades in HCT-116 human colon carcinoma cells via redox signaling.
    Anticancer Agents Med Chem 2017 Oct 26. Epub 2017 Oct 26.
    Daegu University, Kyoungsan, Kyoungbook 712-714. Korea.
    Background: Colon cancer is the second most common cancer to cause death worldwide. About half of colon cancer patients require adjuvant therapy to control relapse following surgical resection. Therefore, abolition of tumor cell progression using an effective chemotherapeutic agent holds a feasible approach to treat patients suffering from colon cancer. Read More

    Oleanolic acid inhibits colorectal cancer angiogenesis by blocking the VEGFR2 signaling pathway.
    Anticancer Agents Med Chem 2017 Oct 20. Epub 2017 Oct 20.
    Xuzhou Central Hospital affiliated to Southeast University. China.
    Angiogenesis is a crucial process that regulated by multiple intracellular signaling pathways including MEK/ERK and JNK/SAPK. Thus, many inhibitors have developed to these pathways as anti‑cancer therapeutic strategies. Oleanolic acid (OA) is a natural pentacyclic triterpenoic acid compound that present in various herbal medicines. Read More

    Dual antibacterial and anticancer activity of 4-benzoyl-1-dichlorobenzoylthiosemicarbazide derivatives.
    Anticancer Agents Med Chem 2017 Oct 23. Epub 2017 Oct 23.
    Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, Chodźki 4a, 20-093 Lublin. Poland.
    A group of 4-benzoyl-1-dichlorobenzoylthiosemicarbazides endowed with antibacterial activity were evaluated towards their cytotoxic properties against breast cancer cells (MCF-7, MDA-MB-231) and head and neck squamous cell carcinomas (FaDu, SCC-25). Cytotoxicity of the investigated compounds was measured using MTT and [3H]-thymidine incorporation bioassays. 1-(2,3-Dichlorobenzoyl)-4-(2-methylbenzoyl)thiosemicarbazide (TA-4), 1-(2,4-dichlorobenzoyl)-4-(2-methylbenzoyl)thiosemicarbazide (TA-18), and 1-(2,4-dichlorobenzoyl)-4-(4-nitrolbenzoyl)thiosemicarbazide (TA-20) were found to possess anticancer activity equipotent or even stronger than that of reference drug - etoposide. Read More

    Research Progress in Reversal of Tumor Multi-drug Resistance via Natural Products.
    Anticancer Agents Med Chem 2017 Oct 16. Epub 2017 Oct 16.
    Key Laboratory of Liver and Kidney Diseases, Institute of Liver Diseases - Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine Shanghai. China.
    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. Read More

    Immunopharmacological activity of betulin in inflammation-associated carcinogenesis.
    Anticancer Agents Med Chem 2017 Oct 12. Epub 2017 Oct 12.
    Institute of General Pharmacology and Toxicology, Immune Pharmacology, pharmazentrum frankfurt/ZAFES, Clinic of the Goethe University , Theodor-Stern-Kai 7, 60590 Frankfurt am Main. Germany.
    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. Read More

    New ferrocene compounds as selective cyclooxygenase (COX-2) inhibitors: design, synthesis, cytotoxicity and enzyme-inhibitory activity.
    Anticancer Agents Med Chem 2017 Oct 3. Epub 2017 Oct 3.
    Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran. Iran.
    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. Read More

    Targeting cell necroptosis and apoptosis induced by Shikonin via receptor interacting protein kinases in estrogen receptor positive breast cancer cell line, MCF-7.
    Anticancer Agents Med Chem 2017 Sep 19. Epub 2017 Sep 19.
    Department of Clinical Biochemistry, Faculty of Medicine, Shahid Beheshti University of Medical Sciences, Tehran. Iran.
    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. Read More

    Anticancer properties of a new hybrid analog AD-013 combining a coumarin scaffold with an α-methylene-δ-lactone motif.
    Anticancer Agents Med Chem 2017 Sep 21. Epub 2017 Sep 21.
    Department of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz. Poland.
    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.

    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. Read More


    The Measurement and Mathematical Analysis of 5-Fu Release from Magnetic Polymeric Nanocapsules, following the Application of Ultrasound.
    Anticancer Agents Med Chem 2017 Sep 21. Epub 2017 Sep 21.
    Medical Physics Department, School of Medicine, Iran University of Medical Sciences (IUMS), Tehran. Iran.
    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. Read More

    Antileukemic Properties of Sesquiterpene Lactones : A systematic review.
    Anticancer Agents Med Chem 2017 Sep 18. Epub 2017 Sep 18.
    Fluminense Federal University - Molecular and Cellular Biology Niterói, Rio de Janeiro. Brazil.
    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). Read More

    Human Fibronectin Extra-Domain B (EDB)-Specific Aptide (APTEDB) Radiolabelling with Technetium-99m as a Potent Targeted Tumour-Imaging Agent.
    Anticancer Agents Med Chem 2017 Sep 18. Epub 2017 Sep 18.
    Pasteur Institute of Iran - North Research Centre Amol, Mazandaran. Iran.
    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. Read More

    Genistein induces alterations of epigenetic modulatory signatures in human cervical cancer cells.
    Anticancer Agents Med Chem 2017 Sep 18. Epub 2017 Sep 18.
    Manipal University - School of Life Sciences Academic City, Dubai,United Arab Emirates Manipal University - School Of Life Sciences Academic City, Dubai. United Arab Emirates.
    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). Read More

    4-aryl/heteroaryl-4H-fused pyrans as Anti-proliferative Agents: Design, Synthesis and Biological Evaluation.
    Anticancer Agents Med Chem 2017 09 18. Epub 2017 Sep 18.
    M.M.College of Pharmacy, M.M.University - Department of Pharmaceutical Chemistry Mullana, Ambala. India.
    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. Read More

    The Antitumor Potential of Marine Natural Products: A Mechanistic Investigation.
    Anticancer Agents Med Chem 2017 Sep 18. Epub 2017 Sep 18.
    Xuyi People's Hospital, Xuyi, Jiangsu. China.
    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. Read More

    Stereocomplexation Assisted Assembly of Poly(g-glutamic acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier.
    Anticancer Agents Med Chem 2017 Sep 11. Epub 2017 Sep 11.
    Wuhan University of Technology - School of Chemistry, Chemical Engineering and Life Sciences Guangzhou. China.
    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. Read More

    Inhibition of proliferation and induction of Apoptosis by Thymoquinone via modulation of TGF family, p53, p21 and Bcl-2α in leukemic cells.
    Anticancer Agents Med Chem 2017 09 12. Epub 2017 Sep 12.
    King Abdulaziz University - Special Infectious Agents Unit; Yousef Abdullatif Jameel Chair of Prophetic Medicine Appli Jeddah. Saudi Arabia.
    Introduction: Adult T-cell leukemia (ATL) is an aggressive form of malignancy caused by human T-cell lymphotropic virus 1 (HTLV-1). Currently, there is no effective treatment for ATL. Thymoquinone has been reported to have anti-cancer properties. Read More

    α-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 ".
    Anticancer Agents Med Chem 2017 Sep 12. Epub 2017 Sep 12.
    Solapur university, Solapur - Chemistry Solapur, Maharashtra. India.
    • 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. Read More

    Novel Findings of Anti-cancer Property of Propofol.
    Anticancer Agents Med Chem 2017 Sep 12. Epub 2017 Sep 12.
    Department of Anesthesiology, Fudan University Shanghai Cancer Center, Shanghai 200032. China.
    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. Read More

    Spices with Breast Cancer Chemopreventive and Therapeutic Potentials: A Functional Foods Based-Review.
    Anticancer Agents Med Chem 2017 Sep 12. Epub 2017 Sep 12.
    Department of Biochemistry, Ahmadu Bello University, Zaria, Kaduna State. Nigeria.
    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. Read More

    VDAC1 mediated anticancer activity of gallic acid in human lung adenocarcinoma A549 cells.
    Anticancer Agents Med Chem 2017 Sep 11. Epub 2017 Sep 11.
    Peking University - Pharmacology department Beijing. China.
    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. Read More

    Structure-Based Drug Design: Synthesis, X-Ray Crystallography, and Biological Evaluation of N-Substituted-4-Hydroxy-2-Quinolone-3-Carboxamides as Potential PI3Kα Inhibitors.
    Anticancer Agents Med Chem 2017 Sep 11. Epub 2017 Sep 11.
    The University of Jordan, Amman 11942. Jordan.
    Background: Oncogenic potential of phosphatidylinositol 3-kinase (PI3Kα) has been highlighted as a therapeutic target for anticancer drug design.

    Objective: Target compounds were designed to address the effect of different substitution patterns at the N atom of the carboxamide moiety on the bioactivity of this series.

    Methods: Synthesis of the targeted compounds, crystallography, biological evaluation tests against human colon carcinoma (HCT-116), and Glide docking studies. Read More

    From biology to therapy: Improvements of therapeutic options in Lung cancer.
    Anticancer Agents Med Chem 2017 Sep 12. Epub 2017 Sep 12.
    University Federico II of Naples. Italy.
    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. Read More

    Molecular characterization of two polysaccharides from Phellinus vaninii Ljup and their anti-tumor activities.
    Anticancer Agents Med Chem 2017 Sep 12. Epub 2017 Sep 12.
    Zhengzhou University of Light Industry. China.
    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. Read More

    Pyramidatine (Z88) Sensitizes Vincristine-Resistant Human Oral Cancer (KB/VCR) Cells to Chemotherapeutic Agents by Inhibition of P- glycoprotein.
    Anticancer Agents Med Chem 2017 Aug 3. Epub 2017 Aug 3.
    State Key Laboratory of Genetic Engineering Institute of Genetics, School of Life Sciences Fudan University, Shanghai 200433. China.
    Multi-drug resistance (MDR) to anticancer drugs remains a major impediment in cancer therapy. A major goal for scientists is to identify more effective compounds that are able to circumvent MDR and simultaneously have minimal adverse side effects. Here, we reported that Pyramidatine (Z88), a cinnamic acid-derived bisamide compound isolated from the leaves of Aglaia perviridis, had potent anti-MDR activity. Read More

    The Application of the Cold Atmospheric Plasma-Activated Solutions in Cancer Treatment.
    Anticancer Agents Med Chem 2017 Jul 31. Epub 2017 Jul 31.
    The George Washington University - Department of Mechanical and Aerospace Engineering Washington, DC. United States.
    Over past five years, the cold atmospheric plasma-activated solutions (PAS) has shown its promissing application in cancer treatment. Similar as the common direct cold plasma treatment, PAS shows a selective anti-cancer capacity in vitro and in vivo. However, different from the direct cold atmospheric plasma (CAP) treatment, PAS can be stored for a long time and can be used without dependence on a CAP device. Read More

    Effects of Plasma Activated Medium on Head and Neck FaDu Cancerous Cells: comparison of 3D and 2D response.
    Anticancer Agents Med Chem 2017 Aug 1. Epub 2017 Aug 1.
    LAPLACE, UPS, Université de Toulouse, Toulouse. France.
    Objective: The aim of this work is to investigate the inhibitory effect of Plasma Activated Medium (PAM) on Head and Neck cancerous cells (FaDu).. The response of FaDu cells in monolayer cultures and Multi Cellular Tumor Spheroids (MCTS) after treatment with different PAMs will be compared. Read More

    Hydrogen peroxide and beyond - the potential of high-voltage plasma-activated liquids against cancerous cells.
    Anticancer Agents Med Chem 2017 08 1. Epub 2017 Aug 1.
    Dublin Institute of Technology - School of Food Science and Environmental Health Dublin. Ireland.
    The use of plasma-activated liquids such as PBS, medium or simply plasma-activated water (PAW) has been receiving increasing attention for applications in cancer treatments. Amongst the reactive species contained in these solutions, hydrogen peroxide appears to play a pivotal role in causing cytotoxic effects. While H2O2 concentrations can be correlated with reduced cell viability and growth and used as an indicator of the potential efficacy of a plasma-activated water, comparisons to standard H2O2 kill curves demonstrate a potency in PAW which exceeds H2O2 associated toxicity, indicating that other plasma-generated species play an important role. Read More

    Targeting protective catalase of tumor cells with cold atmospheric plasma-treated medium (PAM).
    Anticancer Agents Med Chem 2017 Aug 1. Epub 2017 Aug 1.
    Institute of Virology, Hermann-Herder-Strasse 11 D-79104 Freiburg. Germany.
    ● Background Application of cold atmospheric plasma to medium generates "plasma-activated medium" that induces apoptosis selectively in tumor cells and that has an antitumor effect in vivo. The underlying mechanisms are not well understood. ● Objective Elucidation of potential chemical interactions within plasma-activated medium and of reactions of medium components with specific target structures of tumor cells should allow to define the active principle in plasma activated medium. Read More

    Activity of saponins from Medicago species against HeLa and MCF-7 cell lines and their capacity to potentiate cisplatin effect.
    Anticancer Agents Med Chem 2017 Jul 27. Epub 2017 Jul 27.
    DISTEBA, Università del Salento, Via Monteroni, 73100 Lecce. Italy.
    In the present paper we aim to describe the cytotoxic properties of saponin mixtures from M. arabica (tops and roots), M. arborea (tops) and M. Read More

    Effect of number of bifunctional chelating agents on the pharmacokinetics and immunoreactivity of 177Lu-labeled Rituximab: A systemic study.
    Anticancer Agents Med Chem 2017 Jul 25. Epub 2017 Jul 25.
    Bhabha Atomic Research Centre - Radiopharmaceuticals Division Mumbai. India.
    Objective: Monoclonal antibodies (mAbs) have been radiolabeled with a variety of radioisotopes utilizing various kinds of bi-functional chelating agents (BFCAs) with an aim to develop suitable agents for radioimmunotherapy. The number of BFCA moieties present per antibody molecule plays a significant role in determining the pharmacokinetics and immunoreactivity exhibited by the radiolabeled antibodies. The objective of the present study is to evaluate the effect of number of BFCA moieties present per antibody molecule on the pharmacokinetics and immunoreactivity of the 177Lu-labeled Rituximab. Read More

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