Synthesis of Novel Benzothiazole-Piperazine Derivatives and Their Biological Evaluation as Acetylcholinesterase Inhibitors and Cytotoxic Agents.

abstract：BACKGROUND:A monoterpene, perillyl alcohol, has attracted attention in medicinal chemistry since it exhibited chemo-preventive and therapeutic properties against a variety of cancers. OBJECTIVE:In the present work, it was aimed to obtain derivatives of perillyl alcohol through microbial biotransformation and investiga...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Oturanel CE,Kıran İ,Özşen Ö,Çiftçi GA,Atlı Ö

更新日期：2017-01-01 00:00:00

abstract：:As chemotherapy with temozolomide is far from providing satisfactory clinical outcomes for patients with glioblastoma, more efficient drugs and drug combinations are urgently needed. The anti-malarial artesunate was previously shown to exert a profound cytotoxic effect on various tumor cell lines including those deriv...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Karpel-Massler G,Westhoff MA,Kast RE,Dwucet A,Nonnenmacher L,Wirtz CR,Debatin KM,Halatsch ME

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND:T-LAK cell-originated protein kinase (TOPK) belongs to the serine/threonine protein kinase family. It is highly expressed in RPMI7951 melanoma cells. Scutellarin (SCU) is an active ingredient extracted from Erigeron breviscapus (Vant.) Hand.-Mazz. Its main physiological functions are related to its anti-infl...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Mu X,Wang L,Zhang Z,Ge R,Zhang J,Mou K,Liu W,Lv S

更新日期：2020-08-10 00:00:00

abstract：:A novel process for the preparation of two ketomethylenic antifolates, 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-amino]- phenyl}-2-oxo-ethyl) pentanedioic acid and 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-phenyl}-2-oxo-ethyl) pentanedioic acid is described herein. Both compounds were compared with met...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Stoicescu DF,Rotaru M

更新日期：2013-02-01 00:00:00

abstract：BACKGROUND:The existence of drug-resistance and lack of selectivity encourages scientists to search for novel and more selective cytotoxic agents. OBJECTIVES:In this work, novel 1,3,4-triarylpyrazole derivatives were synthesized to study their cytotoxicity on MCF7 (human breast Cell Line). In addition, QSAR studies we...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Ismail MMF,Farrag AM,Harras MF

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Cancer is the second leading cause of mortality worldwide. Despite several advances made in the treatment strategies, the cure for cancer remains still a challenge. Currently used treatment modalities pose several side effects and remain ineffective in the later stages. Thiazolidinediones (TZDs) have been sh...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Uwabagira N,Sarojini BK,Prabhu A

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Edible and medicinal plants are still an interesting source of promising biologically active substances to drug discovery and development. At a time of increasing cancer incidence in the world, alleviating the bothersome side effects of radiotherapy in debilitated cancer patients is becoming an important cha...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Karpiński TM,Adamczak A,Ożarowski M

更新日期：2020-10-29 00:00:00

abstract：AIM:The aim of our research work is the synthesis of tetrahydroisoquinoline derivatives as anti-Angiogenesis and anti-cancer agents. BACKGROUND:Cancer is the second leading cause of deaths in United States. The current recovery rate from the advanced treatment for the cancer is unacceptably low. Therefore, identificat...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Gangapuram M,Eyunni S,Zhang W,Redda KK

更新日期：2021-01-12 00:00:00

abstract：:A concept that currently steers the development of cancer therapies has been that agents directed against specific proteins that facilitate tumorigenesis or maintain a malignant phenotype will have greater efficacy, less toxicity and a more sustained response relative to traditional cytotoxic chemotherapeutic agents. ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Driscoll JJ,Minter A,Driscoll DA,Burris JK

更新日期：2011-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:The ratio of live cells to total cells in a sample is a definition for cell viability or cell toxicity. The assessment of the viable cells plays a critical role in all processes of the cell culture workflows. Overall, they are used to evaluate the survival of cells and also to optimize culture ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Nozhat Z,Khalaji MS,Hedayati M,Kia SK

更新日期：2020-12-30 00:00:00

abstract：BACKGROUND:Targeted imaging and therapy (theranostics) is a promising approach for the simultaneous improvement of cancer diagnosis, prognosis and management. Therapeutic and imaging reagents are coupled to tumor-targeting molecules such as antibodies, providing a basis for truly personalized medicine. However, the dev...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Chouman K,Woitok M,Mladenov R,Kessler C,Weinhold E,Hanz G,Fischer R,Meinhold-Heerlein I,Bleilevens A,Gresch G,Haugg AM,Zeppernick F,Bauerschlag D,Maass N,Stickeler E,Kolberg K,Hussain AF

更新日期：2017-01-01 00:00:00

abstract：:Phospholipase A2 (PLA2), Cyclooxygenase (COX) and 5-Lipoxygenase (5-LOX) are arachidonic acid metabolizing enzymes and their inhibitors have been developed as therapeutic molecules for cancer and inflammation related disorders. In the present study, PLA2, COX 1&2 and 5-LOX inhibitory studies of Borassus flabellifer se...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Yarla NS,Azad R,Basha M,Rajack A,Kaladhar DS,Allam BK,Pragada RR,Singh KN,K SK,Pallu R,Parimi U,Bishayee A,Duddukuri GR

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Cassane-type diterpenoids are widely distributed in the medical plants of genus Caesalpinia. To date, plenty of cassane diterpenoids have been isolated from the genus Caesalpinia, and some of them were documented to exhibit multiple biological activities. However, the effects of these compounds on autophagy ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Zhang LL,Bao H,Xu YL,Jiang XM,Li W,Zou L,Lin LG,Lu JJ

更新日期：2020-01-01 00:00:00

abstract：:Because invasion is, either directly or via metastasis formation, the main cause of death in cancer patients, development of efficient anti-invasive agents is an important research challenge. We have established a screening program for potentially anti-invasive compounds. The assay is based on organotypic confronting ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Bracke ME,Vanhoecke BW,Derycke L,Bolca S,Possemiers S,Heyerick A,Stevens CV,De Keukeleire D,Depypere HT,Verstraete W,Williams CA,McKenna ST,Tomar S,Sharma D,Prasad AK,DePass AL,Parmar VS

更新日期：2008-02-01 00:00:00

abstract：:Glioblastoma (GBM), the most common primary brain tumor in adults, is one of the most aggressive human cancers associated with high mortality. Standard treatments following diagnosis include surgical resection, radiotherapy and adjunctive chemotherapy. However, almost all patients develop disease progression following...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Sathornsumetee S

更新日期：2011-10-01 00:00:00

abstract：:Compounds that can bind and stabilize non-canonical DNA structures are named quadruplex and are of interest in anticancer drug design due to their selective inhibitions of telomerase and consequent effects on cell proliferation. In this study, we report novel Co/Cu [II] complex compounds as G-quadruplex DNA binding li...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Saour K,Lafta D

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Tumor recurrence and metastasis are still leading causes of cancer mortality worldwide. The influence of traditional treatment strategies against metastatic tumors may still be limited. To search for novel and powerful agents against tumors has become a major research focus. In this study, Artemisinin (ARM),...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Li Y,Zhou X,Liu J,Yuan X,He Q

更新日期：2020-01-01 00:00:00

abstract：:Epigenetic modifications can affect numerous mechanisms used by neoplastic cells to evade immune control. In melanoma epigenetic defects, caused by dysregulations in the expression of genome writers, erasers, or readers, play a significant role in the reduced expression of molecules required for efficient immune recog...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Venza M,Visalli M,Catalano T,Beninati C,Teti D,Venza I

更新日期：2017-01-01 00:00:00

abstract：:The systematic improvement of methods used for unraveling physiological and pathological role of proteases, as well as for elucidation of relevant hydrolase structures contributes to the progress in the area of new inhibitor-like drugs development. Many of protease inhibitors have entered clinics and are now successfu...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Białas A,Kafarski P

更新日期：2009-09-01 00:00:00

abstract：BACKGROUND:Cinnamic acid (CA), also known as 3-phenyl-2-propenoic acid, is a naturally occurring aromatic fatty acid found commonly in cinnamon, grapes, tea, cocoa, spinach and celery. Various studies have identified CA to have anti-proliferative action on glioblastoma, melanoma, prostate and lung carcinoma cells. OBJ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Pal A,Tapadar P,Pal R

更新日期：2020-08-07 00:00:00

abstract：:Radiolabelled peptides have shown to be an important class of radiopharmaceuticals for imaging and therapy of malignancies expressing receptors of regulatory peptides. These peptides have high affinity and specificity for their receptors. The majority of these receptors are present at different levels in different tis...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Breeman WA,Kwekkeboom DJ,de Blois E,de Jong M,Visser TJ,Krenning EP

更新日期：2007-05-01 00:00:00

abstract：BACKGROUND:Liposomes have been employed to improve pharmacokinetics and reduce side effects of drugs. They can be functionalized with antibodies for targeted delivery. While the monoclonal antibody trastuzumab has been employed in the therapy of HER2-positive breast cancer, the resistance developed during treatment has...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Eloy JO,Petrilli R,Brueggemeier RW,Marchetti JM,Lee RJ

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:Pyrazole derivatives have been reported as both anticancer and antiinflammatory agents. OBJECTIVE:This study was conducted to develop new pyrazole derivatives as potential anticancer and/or antiinflammatory agents. Their molecular mechanisms of action have been investigated. METHOD:a series of new triarylp...

journal_title：Anti-cancer agents in medicinal chemistry

authors： El-Gamal MI,Abdel-Maksoud MS,Gamal El-Din MM,Shin JS,Lee KT,Yoo KH,Oh CH

更新日期：2017-01-01 00:00:00

abstract：:β-Glucans are polysaccharides of β-D-glucose extracted from the cell walls of different species of mushrooms, yeast, oat, barley, seaweeds, algae and bacteria. Modern biomedical research has identified β-glucans as biological response modifiers (BRM) with anti-tumor properties that elicit potent immune responses throu...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Albeituni SH,Yan J

更新日期：2013-06-01 00:00:00

abstract：:In recent years, there has been an expansion of the understanding of how epigenetic dysregulation plays a role in tumorigenesis, progression, metastasis and treatment resistance. Evidence has focused on two common and well-studied "epigenetic codes", i.e., DNA methylation and histone posttranslational modification, wh...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Jin P,Chen X

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Araucaria angustifolia extract (AAE) is a polyphenol-rich extract that has gained interest as a natural anticancer agent. Recent work suggests that AAE induces oxidative damage and apoptosis through its action on decreasing complex I activity of the mitochondrial Electron Transport Chain (ETC). AIMS AND MET...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Branco CS,Duong A,Machado AK,Scola G,Andreazza AC,Salvador M

更新日期：2019-01-01 00:00:00

abstract：:Evidence supports that a variety of cancers are sparked by the growth of cells that exhibit characteristics of stem cells. Such cancer-initiating cells are capable of populating a tumor with a heterogeneous group of daughter cells while still maintaining the ability to self-renew. Several groups have recently reported...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Murphy SK

更新日期：2010-02-01 00:00:00

abstract：BACKGROUND:Acute myeloid leukemia is the collective name for different types of leukemias of myeloid origin affecting blood and bone marrow. The overproduction of immature myeloblasts (white blood cells) is the characteristic feature of AML, thus flooding the bone marrow and reducing its capacity to produce normal bloo...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Dogra R,Bhatia R,Shankar R,Bansal P,Rawal RK

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:The present study was carried out to evaluate the anticancer property of an alkylamino phenol derivative -2-((3,4-Dihydroquinolin-1(2H)-yl)(p-tolyl)methyl)phenol) (THTMP) against human breast cancer cells. The cytotoxicity of the THTMP was assessed to know its specificity towards breast cancer ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Palanivel S,Yli-Harja O,Kandhavelu M

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Peniciketal A (Pe-A), a spiroketal compound, shows potent anticancer activities in human acute monocytic leukemia. However, the detailed mechanisms and potent targets of Pe-A remain largely unexplored. Here, we investigated the differentially expressed proteins between the Pe-A-treated group and the control ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Gao X,Zhou Y,Sun H,Liu D,Zhang J,Zhang J,Liu W,Pan X

更新日期：2019-01-01 00:00:00