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    1443 results match your criteria Anti-Cancer Agents in Medicinal Chemistry[Journal]

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    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 Sep 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 Sep 12. Epub 2017 Sep 12.
    King Abdulaziz University - Special Infectious Agents Unit; Yousef Abdullatif Jameel Chair of Prophetic Medicine Appli Jeddah. Saudi Arabia.
    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. 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 Aug 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

    Anethole Inhibits The Proliferation Of Human Prostate Cancer Cells Via Induction Of Cell Cycle Arrest And Apoptosis.
    Anticancer Agents Med Chem 2017 Jul 25. Epub 2017 Jul 25.
    Zoology Department, Faculty of Science, Alexandria University, Alexandria, Egypt Department of Biological Sciences, Faculty of Sciences, King Abdulaziz University, Jeddah. Saudi Arabia.
    Background: Prostate cancer-associated mortality is increasing at an alarming rate, which highlights the inevitability for unearthing novel agent for the management of this disease. Anethole, a major constituent of Foeniculum vulgare (fennel) essential oil, is widely used in folk medicine; it possesses anti-oxidant, anti-inflammatory, anti-proliferative and tumoricidal potentialities.

    Objective: The current research was conducted to assess the impact of anethole on prostate cancer cell line, PC-3, and to delineate the molecular mechanism of action. Read More

    Synthesis of Pyridine and Spiropyridine derivatives derived from 2-aminoprop-1-ene-1,1,3-tricarbonitrile together with their c-Met kinase and antiproliferative evaluations.
    Anticancer Agents Med Chem 2017 Jul 25. Epub 2017 Jul 25.
    Faculty of Science, Helwan University - pharmaceutical Chemistry Cairo. Egypt.
    Objective/method: The multi-component reaction of 2-aminoprop-1-ene-1,1,3-tricarbonitrile (1) with aromatic aldehydes 2a-c and malononitrile (3a) or ethyl cyanoacetate (3b) to give the pyridine derivatives 5a-f. Compounds 5a-c were found to react with either hydrazine hydrate (6a) or phenylhydrazine (6b) to give 2-pyrazolylpyridine derivatives 7a-f, respectively. On the other hand, compound 1 reacted with cyclopentanone (8a) or cyclohexanone (8b) and malononitrile (3a) or ethyl cyanoacetate (3b) to give the spiro derivatives 9a-d, respectively. Read More

    Effects of Ascorbic Acid on Tax, NF- κB and MMP-9 in Human T-cell Lymphotropic virus type 1 positive malignant T-Lymphocytes.
    Anticancer Agents Med Chem 2017 Jul 25. Epub 2017 Jul 25.
    Dr. Rath Research Institute Santa Clara, California,United States Dr. Rath Research Institute Santa Clara, CA. United States.
    Background: HTLV-1 is a retrovirus that infects CD4-positive cells and leads to Adult T-cell leukemia by constitutive activation of nuclear factor kappa B. Ascorbic acid (AA) is an essential nutrient that possess anti-proliferative and pro-apoptotic activity against a number of malignant cell lines. This study delineates the effect of AA on Tax protein expression as well as NF-κB and MMP9 activity in two HTLV-1-positive leukemia cells (HuT-102 and C91-PL). Read More

    CCL2 is Modulated by Cytokines and PPAR-g in Anaplastic Thyroid Cancer.
    Anticancer Agents Med Chem 2017 Jul 19. Epub 2017 Jul 19.
    University of Pisa - Department of Clinical and Experimental Medicine Pisa. Italy.
    Background And Objective: Chemokine (C-C motif) ligand (CCL)2, the prototype Th2 chemokine, is secreted by tumor cells, and has growth promoting effects. Whether CCL2 protumorigenic activities will be validated, then CCL2 and its receptor CCR2 may be therapeutic targets in cancer.

    Methods: We tested in "primary human anaplastic thyroid carcinoma (ATC) cells" (ANA) versus "normal thyroid follicular cells" (TFC): a) CCL2 secretion basally, after IFN-g and/or TNF-a stimulation; b) PPARg activation by thiazolidinediones (TZDs), rosiglitazone or pioglitazone, on CCL2 secretion, and on proliferation and apoptosis in ANA. Read More

    Increased expression of IRE1α associates with the resistant mechanism of osimertinib (AZD9291)-resistant non-small cell lung cancer HCC827/OSIR cells.
    Anticancer Agents Med Chem 2017 Jul 19. Epub 2017 Jul 19.
    State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao. China.
    Background: Osimertinib (OSI), also known as AZD9291, is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that has been approved for the treatment of non-small cell lung cancer (NSCLC) patients.

    Objective: Establishment of the OSI-resistant HCC827/OSIR cell line and study of its resistant mechanism.

    Method: The anti-proliferative effect was studied through MTT and colony formation assays. Read More

    Phosphonium Salt Displays Cytotoxic Effects Against Human Cancer Cell Lines.
    Anticancer Agents Med Chem 2017 Jul 19. Epub 2017 Jul 19.
    Department of Science, University of Basilicata, 85100, Potenza Potenza (Pz). Italy.
    Aims/ Objective: Phosphonium salts are compounds whose structural characteristics enable them to cross the plasma and mitochondrial membrane with ease. Cancer cells have higher plasma membrane potentials than normal cells, phosphonium salts selectively accumulate in the mitochondria of neoplastic cells and inhibit mitochondrial function.

    Method: In the presente work, we investigate the cytotoxic activity of lipophilic phosphonium salt (11-methoxy11-oxo-undecyl) triphenylphosphonium bromide (MUTP) as well as of two new phosphine oxide salts, 3,3'-(methylphosphoryl) dibenzenaminium chloride (SBAMPO) and 3,3' (phenylphosphoryl) dibenzenaminium chloride (SBAPPO) on the proliferation of breast cancer cell line (MCF-7) and human uterin cervix adenocarcinoma cells (HeLa). Read More

    Novel Fluorinated Porphyrins Sensitize Tumor Cells to Photodamage in Normoxia and Hypoxia: Synthesis and Biocompatible Formulations.
    Anticancer Agents Med Chem 2017 Jul 19. Epub 2017 Jul 19.
    A.N.Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Moscow. Russian Federation.
    : Background. Hypoxia renders tumor cells refractory to treatment. One way to overcome this problem is the design of drug delivery systems that contain the antitumor agent within an oxygen supply medium. Read More

    Recent progress of nano-drug delivery system for liver cancer treatment.
    Anticancer Agents Med Chem 2017 Jul 13. Epub 2017 Jul 13.
    School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province. China.
    Liver cancer is one of serious diseases which threaten human life and health. Studies on the treatment of liver cancer have attracted widespread attention. Application of nano-drug delivery system (NDDS) can not only improve selective drug delivery to liver tissue and improve the bioavailability of drug, but also can reduce the side effects of drugs when it is specially modified in the respects of structure modification or specific target molecules decoration. Read More

    Synthesis, radiosynthesis, and metabolism of 131I-Y-c(CGRRAGGSC).
    Anticancer Agents Med Chem 2017 Jul 13. Epub 2017 Jul 13.
    Wuxi Hospital for Maternal and Child Health Care Affiliated to Nanjing Medical University, Wuxi, Jiangsu 214002. China.
    Background: The formation of the complex interleukin-11(IL-11) and IL-11 receptor (IL-11R) is closely related with tumor progression. Binding of IL-11 to the IL-11 receptor α-chain (IL-11Rα) has been suggested as a target for human cancer. The cyclic peptide c(CGRRAGGSC) is a mimic of IL-11. Read More

    Design and discovery of novel quinoxaline derivatives as dual DNA intercalators and topoisomerase II inhibitors.
    Anticancer Agents Med Chem 2017 Jul 10. Epub 2017 Jul 10.
    Chemistry Department, Faculty of science, Ain shams University, Abbassia, Cairo, 11566. Egypt.
    In attempt to develop new potent anti-tumor agents, a series of quinoxaline derivatives was designed and synthesized. The novel compounds were tested in vitro for their anti-proliferative activities against HePG-2, MCF-7 and HCT-116 cell lines. Additionally, DNA binding affinities as well as DNA-top II inhibitory activities of the synthesized compounds were investigated as potential mechanism for the anticancer activity. Read More

    Synthesis and evaluation of antioxidant and cytotoxicity of the N-Mannich base of berberine bearing benzothiazole moieties.
    Anticancer Agents Med Chem 2017 Jul 10. Epub 2017 Jul 10.
    Department of Food Science and Biotechnology, Dongguk University-Seoul, Ilsandong-gu, Goyang-si, Gyeonggi-do 410-820. Korea.
    The N-Mannich base of an isoquinoline alkaloid, berberine, bearing substituted benzothiazole moieties was obtained. Novel synthesized analogues were in vitro screened for antioxidant efficacy toward 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) free radicals and in vitro cytotoxicity towards cervical cancer cell lines (HeLa and CaSki), an ovarian cancer cell line (SK-OV-3) and human renal cancer cell line (Caki-2). Cytotoxicity of the compounds toward normal cell lines was examined using the Madin-Darby canine kidney (MDCK) non-cancer cell line. Read More

    Evaluation of Multifunctional Hybrid Analogs for Stilbenes, Chalcones and Flavanones.
    Anticancer Agents Med Chem 2017 May 29. Epub 2017 May 29.
    Department of Biology, Faculty of Science, Anadolu University, Eskisehir. Turkey.
    Eleven simple-stilbene, chalcone, flavanone derivatives and 31 novel stilbene-fused chalcones and stilbene-fused flavanones were tested for their aromatase inhibition, anti-angiogenic and anti-proliferative properties in cancer (PC3, MCF-7) and healthy (HUVEC) cell lines. Results indicate that the simple-chalcone and flavanone derivatives were more cytotoxic than the simple-stilbenes in the both cancer cell lines. In contrast, the simple-stilbene structures were much more effective at aromatase inhibition. Read More

    A comparison of the toxicity of mono, bis, tris and tetrakis phosphino silver complexes on SNO esophageal cancer cells.
    Anticancer Agents Med Chem 2017 May 22. Epub 2017 May 22.
    University of Johannesburg - Biochemistry Auckland Park. South Africa.
    Several silver(I) triphenylphosphine adducts were prepared as 1:1 to 1:4 ratios of silver nitrate to triphenylphosphine were used to determine their anticancer activity in a malignant SNO esophageal cell line. The silver-phosphine adducts include: [Ag(PPh3)]NO3 (1); [Ag(PPh3)2]NO3 (2); [Ag(PPh3)3]NO3 (3) and [Ag(PPh3)4]NO3 (4). In addition, the activity of 1-4 where compared to previously reported complexes [Ag(Ph2P(CH2)2PPh2)2]NO3 (5) and [Ag(Ph2P(CH2)3PPh2)2]NO3 (6). Read More

    Synthesis of new antibacterial Cubane-based nanocomposite and its application in combination cancer therapy.
    Anticancer Agents Med Chem 2017 May 22. Epub 2017 May 22.
    Chemistry Department, Azarbaijan Shahid Madani University, Tabriz. Iran.
    Background: The need for therapeutically effective anticancer drug delivery systems constantly persuades researchers to explore novel strategies.

    Objective: In this study a novel cubane based antibacterial nanocomposite was tailored as dual chemotherapy drug delivery vesicle in order to increase the therapeutic outcome in cancer therapy.

    Method: The physico-chemical characterization of engineered nanocarrier was assessed by Fourier transforms infrared spectroscopy (FTIR), Hydrogen nuclear magnetic resonance spectroscopy (1H NMR), Thermogravimetric analysis (TGA), and Field emission scanning electron microscopy-energy dispersive using X-ray (FESEM-EDX). Read More

    Novel N-mustard-benzimidazoles/benzothiazoles hybrids, synthesis and anticancer evaluation.
    Anticancer Agents Med Chem 2017 May 22. Epub 2017 May 22.
    Institute of Biomedical Sciences, Academia Sinica, Taipei 115. Taiwan.
    Background: Bendamustine, an N-mustard-benzoimidazole hybrid conjugate, was recently approved for the treatment of chronic lymphocytic leukemia. However, the short half-life of bendamustine may limit its clinical applications.

    Objective: The purpose of this study is to design and synthesize compounds with a more favorable pharmacokinetic profile. Read More

    1,3,4-Oxadiazoles as telomerase inhibitor: Potential anticancer agents.
    Anticancer Agents Med Chem 2017 Apr 24. Epub 2017 Apr 24.
    Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur- 495009, Chhattisgarh . India.
    Cancer is a rapidly growing disease of current era which poses a major life threaten situation to human beings. Continuous research is going on in the direction to develop effective molecules for the treatment of the cancer. These efforts include searching of more active heterocyclic compounds possessing potential anti-cancer activity. Read More

    Synergistic effect of graphene oxide coated nanotised apigenin with paclitaxel (GO-NA/PTX): A ROS dependent mitochondrial mediated apoptosis in ovarian cancer.
    Anticancer Agents Med Chem 2017 Apr 24. Epub 2017 Apr 24.
    Photobiology Division, CSIR-Indian Institute of Toxicology Research, Post Box No. 80, M.G. Marg, Lucknow, 226001. India.
    Ovarian cancer is most lethal among all gynecologic malignancies. Paclitaxel (PTX) is well used chemotherapeutic regimen for cancer control; however its undesired toxicity has been always a matter of concern for clinicians. Here we used the graphene oxide coated nanotised apigenin (GO-NA) as chemo sensitizing agent to enhance the efficacy of paclitaxel to overcome the limitations of chemotherapy. Read More

    Synthesis, characterization, and inducing tumor cell apoptosis of two Ru(II) complexes containing guanidinium as ligands.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    School of Pharmacy, Guangdong Medical University, Dongguan, 523808. China.
    Two new ruthenium(II) complexes containing guanidinium as ligands, [Ru(dip)2(L1)]3+ (Ru1) and [Ru(dip)2(L2)]3+ (Ru2) (dip = 4,7-diphenyl-1,10-phenanthroline; L1 = 1-(4-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation; L2 = 1-(3-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation) have been synthesized and characterized. Both complexes display higher cytotoxicity against several cancer cell lines compared to cisplatin and are less cytotoxic on the nontumorigenic cell line LO2. Intracellular distribution studies show that these complexes are selectively localized in the cytoplasm. Read More

    Nano-encapsulation of dietary phytoconstituent capsaicin on emulsome: evaluation of anticancer activity through the measurement of liver oxidative stress in rats.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    NSHM College of Pharmaceutical Technology, NSHM Knowledge Campus, Kolkata Group of Institutions, 124 BL Saha Road, Kolkata-700053, West Bengal. India.
    Protective effects of capsaicin (CAP) loaded nano-emulsomes (EML) was evaluated against the oxidative stress of rat livers induced through sodium fluoride (NaF). EML was prepared by thin film hydration method that is development of thin lipid film followed by hydration and sonication. EML was characterized by Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) techniques. Read More

    Antioxidant properties of fractions for unripe fruits of Capsicum annuum L. var. conoides.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    Kaohsiung Medical University - Department of Biomedical Science and Environmental Biology Kaohsiung. Taiwan.
    Background: Capsicum plant, especially for C. annuum, is an abundant resource for bioactive antioxidants, but few studies have examined the unripe fruit part of the Capsicum plant.

    Objective: MeOH extract of unripe fruits of C. Read More

    Apicidin Inhibited Proliferation and Invasion and Induced Apoptosis via Mitochondrial Pathway in Non-small Cell Lung Cancer GLC-82 Cells.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    School of Pharmaceutical Sciences,Guangzhou Medical University, Guangzhou 511436. China.
    Apicidin, an inhibitor of histone deacetylase obtained from the mangrove endophytic fungi Fusarium sp., showed a wide range of antiproliferative activity against various cancer cell lines. Apicidin has also been reported to induce apotosis via Fas/Fas ligand. Read More

    Tumor-targeting peptides: ligands for molecular imaging and therapy.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    Department of Radiology, Molecular Imaging Program at Stanford (MIPS), Bio-X Program and Stanford Cancer Center, Stanford University School of Medicine, Stanford, CA, 94305. United States.
    The aberrant proliferation of tumor cells and abundant vasculature in tumor tissues are closely correlated with receptors that are specifically dysregulated in tumor cells. These tumor-associated targets are critical in early diagnosis and therapy selection. Ligands such as antibodies, proteins, polypeptides and polysaccharides that specifically bind to these targets can significantly improve the detection and cure rate when used as tumor imaging probes or anti-tumor agents. Read More

    Rationale design, synthesis, cytotoxicity evaluation, and molecular docking studies of 1,3,4-oxadiazole analogues.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    Department of Chemistry, College of Science and Humanity, Prince Sattam Bin Abdulaziz University, P.O. Box 83, Al-Kharj 11942. Saudi Arabia.
    We report herein, the synthesis of two new series of oxadiazole analogues, and their cytotoxicity evaluation. The oxadiazole analogues (5a-h and 12a-h) were structurally related to the heterocyclic (1,3,4- oxadiazole) linked aryl core of IMC-038525 (tubulin polymerization inhibitor), NSC 776715, and NSC 776716, with further modification by incorporating methylene linker. The title compounds (5a-h and 12a-h) were synthesized in good yields, and were characterized by IR, NMR, and mass spectral data. Read More

    Evaluation of the in vitro chemosensitivity and correlation with clinical outcomes in lung cancer using the ATP-TCA.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    The First Affiliated Hospital of Soochow University - Department of Clinical Pharmacology Research Lab Suzhou, Jiangsu. China.
    Background And Objective: Multiple drug resistance (MDR) to chemotherapeutic agents often leads to a failure to respond to chemotherapy. We utilized an in vitro chemosensitivity test to identify sensitive and effective chemotherapeutic drugs and further elucidated the correlation between the in vivo chemosensitivity and clinical outcomes.

    Methods: Here, we evaluated the in vitro chemosensitivity and MDR of 120 lung cancer patients to eight single-drug chemotherapies and of 291 lung cancer patients to seven chemotherapy regimens using an ATP-based tumour chemosensitivity assay (ATP-TCA). Read More

    Discovery of Novel 2-Amino-5-(Substituted)-1,3,4-Thiadiazole Derivatives: New Utilities for Colon Cancer Treatment.
    Anticancer Agents Med Chem 2017 Apr 19. Epub 2017 Apr 19.
    Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow-226025. India.
    In this study, we designed and synthesized (VR1 to VR35) a novel series of 1,3,4-thiadiazole derivatives from 2-amino-5-(substituted)-1,3,4-thiadiazole condensed with substituted aldehyde or ketone in the presence of glacial acetic acid via Wolff-Kishner reduction. Further, synthesized compounds were characterized by FTIR, NMR (1H and 13C), MS and elemental analyses. Before the synthesis, docking studies were performed using various molecular targets of colon cancer like IL-2, IL-6, COX-2, caspase-3, and caspase-8. Read More

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