Design and Synthesis of Tetrahydroisoquinoline Derivatives as AntiAngiogenesis and Anti-Cancer Agents.

abstract：BACKGROUND:Multi-kinase inhibitor sorafenib showed dramatic effects in acute myeloid leukemia (AML) cells harboring fms-related tyrosine kinase 3-internal tandem duplication (FLT3-ITD) mutation. However, FLT3-ITD mutation only occurs in 25% of AML cases. The therapeutic effects of sorafenib in AML patients without FLT3...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Yang N,Gu Z,Liu Z,Huang W,Wang S,Wang L,Gao C

更新日期：2018-01-01 00:00:00

abstract：:Protein kinase B (PKB or Akt) is a central component of the PI3K - PKB - mTOR signalling cascade and is firmly established as an attractive target for pharmacological intervention in cancer. A number of small molecule inhibitors with well-defined, direct molecular interactions with PKB are now known, covering a range ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Collins I

更新日期：2009-01-01 00:00:00

abstract：:Garlic (Allium sativam L.) is widely used in traditional herbal remedies and alternative medicine. The potential health benefits of garlic are largely attributed to its metabolic byproducts. Extensive in vivo and in vitro studies has demonstrated that the garlic derivatives possess anti-cancer effects, but the underly...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Cao HX,Zhu KX,Fan JG,Qiao L

更新日期：2014-01-01 00:00:00

abstract：:In the present review, the discovery and development of quinazoline as tyrosine kinase inhibitors has been described. The synthesis of most potent quinazoline inhibitors of EGFR, VEGFR and PDGRF has been discussed. Structure activity relationship for quinazoline as tyrosine kinase inhibitors has been established. It w...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Srivastava SK,Kumar V,Agarwal SK,Mukherjee R,Burman AC

更新日期：2009-03-01 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：:The kinesin spindle protein (KSP, also known as Hs Eg5) plays an essential part in the proper separation of spindle poles and the correct formation of bipolar mitotic spindle during mitosis. Inhibition of this protein results in cells apoptosis followed by mitotic arrest and the formation of characteristic monoaster s...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Zhang Y,Xu W

更新日期：2008-08-01 00:00:00

abstract：:Despite being long lived, anthracyclines remain the "evergreen" drugs in clinical practice of oncology, showing a potent effect in inhibiting cell growth in many types of tumors, including brain neoplasms. Unfortunately, they suffer from a poor penetration into the brain when intravenously administered due to multidru...

journal_title：Anti-cancer agents in medicinal chemistry

authors： da Ros M,Iorio AL,Lucchesi M,Stival A,de Martino M,Sardi I

更新日期：2015-01-01 00:00:00

abstract：:This article aims to give an overview on etiology, diagnosis and treatment options of osteonecrosis of the jaw bone among cancer patients receiving anti-resorptive drugs (ARDs). The physiologic bone function of continuous resorption and buildup is modified by the use of ARDs. Although ARDs proved to reduce pain and to...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Borumandi F,Aghaloo T,Cascarini L,Gaggl A,Fasanmade K

更新日期：2015-01-01 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：:Sphingolipids are membrane lipids that play important roles in the regulation of cell functions and homeostasis. Alterations in their metabolism have been associated with several pathologies. For this reason, therapeutic strategies based on the design of small molecules to restore sphingolipid levels to their physiolo...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Delgado A,Fabrias G,Bedia C,Casas J,Abad JL

更新日期：2012-05-01 00:00:00

abstract：:A novel triazole nucleoside analogue was discovered to exhibit potent anticancer activity in prostate cancer cells via down-regulating heat shock factor 1 (HSF1) and related heat shock proteins, along with the consequential inhibition of androgen receptor (AR) expression and transactivation, arresting the cell cycle i...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Xia Y,Wang M,Beraldi E,Cong M,Zoubeidi A,Gleave M,Peng L

更新日期：2015-01-01 00:00:00

abstract：:Hepatocellular carcinoma (HCC) is the third most common cause of cancer-related mortality in the world because current treatments, including both surgical and non-surgical ones, cannot effectively cure this disease. Increasing evidence has revealed the importance of cancer stem cells (CSCs) in hepatocarcinogenesis, an...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Lau CK,Yang ZF,Fan ST

更新日期：2011-07-01 00:00:00

abstract：:The therapeutic potential of targeting p21-Activated Kinases (PAK1 - 6) for the treatment of cancer has recently gained traction in the biotech industry. Many pharmaceutically-viable ATP competitive inhibitors have been through different stages of pre-clinical development with only a single compound evaluated in human...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Senapedis W,Crochiere M,Baloglu E,Landesman Y

更新日期：2016-01-01 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:While Thioredoxin Reductase (TrxR) plays an important role in regulation of the intracellular redox balance and various signalling pathways, Glutathione S-Transferase (GSTs) enzymes belong to the detoxification family that catalyse the conjugation of glutathione with various endogenous and xenobiotic electro...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Ozgencli I,Kilic D,Guller U,Ciftci M,Kufrevioglu OI,Budak H

更新日期：2018-01-01 00:00:00

abstract：:Backgroun/Methods: 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...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Eissa IH,El-Naggar AM,El-Sattar NEAA,Youssef ASA

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:The DNA repair enzyme tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a current inhibition target to improve the efficacy of cancer chemotherapy. Previous studies showed that compounds combining adamantane and monoterpenoid fragments are active against TDP1 enzyme. This investigation is focused on th...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Mozhaitsev ES,Zakharenko AL,Suslov EV,Korchagina DV,Zakharova OD,Vasil'eva IA,Chepanova AA,Black E,Patel J,Chand R,Reynisson J,Leung IKH,Volcho KP,Salakhutdinov NF,Lavrik OI

更新日期：2019-01-01 00:00:00

abstract：:Acetogenins (ACG) are naturally occurring compounds that are chemically one of the least investigated families. In the review, we have provided a comprehensive listing of 133 of these compounds for which anti-tumor activity has been documented within the literature. We have compiled and studied their chemical structur...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Mangal M,Khan MI,Agarwal SM

更新日期：2015-01-01 00:00:00

abstract：:Of late medicinal plants and functional foods rich in bioactive phytochemicals have received growing attention as potential agents for cancer chemoprevention. Accumulating evidence from epidemiological studies as well as laboratory data supports the anticancer properties of garlic widely used as a medicinal herb and s...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Nagini S

更新日期：2008-04-01 00:00:00

abstract：:A number of N-alkylated 4-anilinofuro[2,3-b]quinoline derivatives were synthesized and evaluated in vitro against PC-3, A549, and MCF-7 cancer cells and M-10 normal human mammary epithelial cells. The known antimitotic CIL-102 was moderately active against the growth of PC-3 prostate cancer cells with an IC50 value of...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Lo WF,Chou YW,Tseng CH,Shiu YH,Chen YW,Yang SC,Chen YL,Lin MF,Tzeng CC

更新日期：2015-01-01 00:00:00

abstract：:Polyphenol-protein interaction (PPI) is reversible in that polyphenol-protein complex can be dissociated and release the free polyphenols. The aim of this study is to evaluate the contribution of polyphenol-protein interaction on improving the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging capacity of polyphe...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Cao H,Chen X,Yamamoto K

更新日期：2012-10-01 00:00:00

abstract：BACKGROUND:Pyrazolo[3,4-d]pyrimidine scaffold was reported to possess potent cytotoxic and CDK2 inhibitory activity as analogue of roscovitine. OBJECTIVE:To design and synthesize novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidine derivatives as bioisosters of roscovitine with potential cytotoxic and CDK2 inhibitory act...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Maher M,Kassab AE,Zaher AF,Mahmoud Z

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Coumarins are naturally occurring plant metabolites and several synthetic coumarin analogues are known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties. Objective; Keeping this promising pharmacological prop...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Kasumbwe K,Venugopala KN,Mohanlall V,Odhav B

更新日期：2017-01-01 00:00:00

abstract：:The phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) pathway is a key regulator of authophagy. Natural products show anticancer activity and often induce apoptosis or autophagy. The crosstalk between these two types of cell death makes autophagy an interesting target since drugs targetin...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Sun H,Wang Z,Yakisich JS

更新日期：2013-09-01 00:00:00

abstract：:Primary liver cancer is one of the most commonly occurring cancers worldwide. Hepatocellular carcinoma (HCC) represents the majority of primary liver cancer and is the 3rd most common cause of cancer-related deaths globally. Survival rates of patients with HCC are dependent upon early detection as concomitant liver dy...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Sokolowski KM,Koprowski S,Kunnimalaiyaan S,Balamurugan M,Gamblin TC,Kunnimalaiyaan M

更新日期：2016-01-01 00:00:00

abstract：:Sphingosine 1-phosphate (S1P) is a bioactive lipid with diverse biological functions, including cell proliferation, differentiation, angiogenesis, chemotaxis, and migration. Many of the activities of S1P are mediated through five closely related G-protein-coupled receptors of the sphingosine-1-phosphate receptor famil...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Watters RJ,Wang HG,Sung SS,Loughran TP,Liu X

更新日期：2011-11-01 00:00:00

abstract：:Natural and synthetic carbazoles, either in a pure substituted or in an annellated substituted form, represent an important and heterogeneous class of anticancer agents, which has grown considerably over the last two decades. Many carbazole derivatives have been tested for cyctotoxic activity, some of them have entere...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Asche C,Demeunynck M

更新日期：2007-03-01 00:00:00

abstract：:Adrenocortical carcinoma (ACC) is a rare but typically aggressive malignancy. Radical surgery remains the potentially curative option. However, about one third of patients initially present with distant metastases. Regarding to chemotherapy, mitotane alone or in combination with cytotoxic drugs should be the first sel...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Xu YZ,Zhu Y

更新日期：2013-02-01 00:00:00

abstract：:Angiogenesis inhibitors have a major role in the treatment of varying cancers today. While originally thought to be independent of resistance, increasing data suggests varying mechanisms that bring about drug resistance, either intrinsically or through adaptation. The role of vascular endothelial growth factor single ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Tavakoli J,Aragon-Ching JB

更新日期：2010-10-01 00:00:00

abstract：:The evasion of cancer cells from the induction of cell death pathways results in the resistance of tumor to current treatment modalities. Therefore, the resistance to cell death, one of the hallmarks of cancer, is a major target in the development of new approaches to selectively affect cancer cells. The complex inter...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Hartman ML,Czyz M

更新日期：2012-10-01 00:00:00