Cilengitide: the first anti-angiogenic small molecule drug candidate design, synthesis and clinical evaluation.

abstract：INTRODUCTION:Esophageal cancer remains an aggressive disease with poor survival rates. FAK and IGF-1R are two important tyrosine kinases important for cell survival signaling and found to be upregulated in esophageal cancer. Our hypothesis is that a novel small molecule compound that disrupts FAK and IGF-1R protein-pro...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Ucar DA,Cox A,He DH,Ostrov DA,Kurenova E,Hochwald SN

更新日期：2011-09-01 00:00:00

abstract：BACKGROUND:Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the dr...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Varshosaz J,Fardshouraki S,Mirian M,Safaeian L,Jandaghian S,Taymouri S

更新日期：2020-01-01 00:00:00

abstract：:High grade gliomas (HGGs) are primary CNS cancers with more than 95% of patients experiencing tumor recurrence following radiation therapy, chemotherapy, and/or an anti-angiogenic therapy. Populations of glioma 'stem-like' cells (GSCs) exist in both proliferative and non-proliferative states and are capable of tumor r...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Gorin FA,Pasupuleti N,Mahajan D,Dugar S

更新日期：2017-01-01 00:00:00

abstract：:Recently, intensive laboratory and preclinical studies have identified and validated therapeutic molecular targets in cancer, particularly the receptor tyrosine kinases, the intracellular pathways, and the genetic and epigenetic alterations, resulting in an unprecedented surge of novel, targeted therapies and therapeu...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Yasui H,Imai K

更新日期：2008-06-01 00:00:00

abstract：:A series of novel thiohydantoin derivatives were synthesized and evaluated for the abilities of inhibiting cell proliferation and prostate specific antigen (PSA) expression in prostate cancer cells. These derivatives selectively inhibited proliferation of AR positive LNCaP cells and PSA expression except compounds 5i ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Liu J,Liu B,Jing Y,Zhao G

更新日期：2016-01-01 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

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：:The respiratory epithelium expresses the cholinergic system including nicotinic receptors (nAChRs). It was reported that normal human bronchial epithelial cells (BEC), which are the precursor for squamous cell carcinomas, and small airway epithelial cells (SAEC), which are the precursor for adenocarcinomas, have sligh...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Grozio A,Catassi A,Cavalieri Z,Paleari L,Cesario A,Russo P

更新日期：2007-07-01 00:00:00

abstract：:MicroRNAs (miRNAs) are emerging as important regulators in various pathobiological processes in cancer. Genistein, as a major isoflavonoid isolated from dietary soybean, possesses a wide variety of biological activities particularly in cancer prevention. However, the molecular mechanisms by which genistein elicits its...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Xu L,Xiang J,Shen J,Zou X,Zhai S,Yin Y,Li P,Wang X,Sun Q

更新日期：2013-09-01 00:00:00

abstract：:Synthetic alkylphospholipids (APLs), exhibit similarity to the platelet-activating factor (PAF). These compounds have antiproliferative effects on tumour cells and can therefore be regarded as a new class of drugs. Unlike classic cytostatic agents, synthetic alkylphospholipids do not interfere with the DNA or the mito...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Semini G,Hildmann A,von Haefen C,Danker K

更新日期：2014-05-01 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：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：: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：: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：: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: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：: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：:The metabolism of alkylating agents is accompanied by the generation of reactive oxygen species. The aim of this study was to treat estrogen receptor-positive and estrogen receptor-negative human breast cancer cells, MCF-7 and MDA-MB-231, respectively, with cisplatin and five different berenil-platinum (II) complexes,...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Agnieszka G,Ewa A,Anna B,Krzysztof B,Monika C,Elżbieta S

更新日期：2014-01-01 00:00:00

abstract：:To search for novel anticancer agents, we designed and synthesized a series of new triazolyl berberine derivatives. The evaluation of all the synthesized compounds and their anticancer activities against a panel of four human cancer cell lines including MCF-7 (breast), MCF-7/ADR (breast), SW-1990 (pancreatic), SMMC-77...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Jin X,Yan L,Li HJ,Wang RL,Hu ZL,Jiang YY,Cao YB,Yan TH,Sun QY

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND & PURPOSE:In evaluating new drugs for the treatment of various types of cancer, investigations have been made to discover a variety of anti-tumor compounds with less side effects on normal cells. Investigations have shown that the heterodimers S100A8 and S100A9 inhibit the enzyme casein kinase 2 and then pre...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Charkhizadeh S,Imani M,Gheibi N,Shabaani F,Nikpajouh A,Rezvany MR

更新日期：2020-01-01 00:00:00

abstract：:A solid tumour forms an organ-like structure that is comprised of cancer cells as well as stroma cells (fibroblasts, inflammatory cells) that are embedded in an extracellular matrix and are nourished by vascular network. However, tumoral microenvironment is heterogeneous due to the abnormal vasculature network and hig...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Cosse JP,Michiels C

更新日期：2008-10-01 00:00:00

abstract：:Tea catechins exhibit a broad range of pharmacological activities that impart beneficial effects on human health. Epigallocatechin-3-gallate (EGCG), one of the major tea catechins, has been widely associated with cancer prevention and treatment. In addition, tea catechins in combination with anticancer drugs are being...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Shang W,Lu W,Han M,Qiao J

更新日期：2014-01-01 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：BACKGROUND:Colorectal cancer is among the leading causes of death worldwide. The incidence of deaths is expected to be 11.4 million in 2030. OBJECTIVE:We aimed to evaluate the in vitro and in vivo antioxidant and antitumor activities of a novel Bithiophene- Fluorobenzamidine (BFB) against DMH-induced colorectal cancer...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Abdel-Rasol M,El-Beih NM,Yahya SMM,Ismail MA,El-Sayed WM

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:The network interactions link human disease proteins to regulatory cellular pathways leading to better understanding of protein functions and cellular processes. Revealing the network of signaling pathways in cancer through protein-protein interactions at molecular level enhances our understanding of Hepatoc...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Ranjpour M,Katare DP,Wajid S,Jain SK

更新日期：2018-01-01 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

abstract：BACKGROUND:Cancer stem cells (CSC) are subpopulation within the tumor that acts a part in the initiation, progression, recurrence, resistance to drugs and metastasis of cancer. It is well known that epigenetic changes lead to tumor formation in cancer stem cells and show drug resistance. Epigenetic modulators and /or t...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Erkisa M,Aztopal N,Erturk E,Ulukaya E,Yilmaz VT,Ari F

更新日期：2020-12-06 00:00:00

abstract：BACKGROUND:Small Cell Lung Cancer (SCLC) is a highly aggressive malignancy. MYC family oncogenes are amplified and overexpressed in 20% of SCLCs, showing that MYC oncogenes and MYC regulated genes are strong candidates as therapeutic targets for SCLC. c-MYC plays a fundamental role in cancer stem cell properties and ma...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Tokgun O,Tokgun PE,Inci K,Akca H

更新日期：2020-01-01 00:00:00

abstract：:Replication fork reversal and restart has gained immense interest as a central response mechanism to replication stress following DNA damage. Although the exact mechanism of fork reversal has not been elucidated precisely, the involvement of diverse pathways and different factors has been demonstrated, which are centr...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Jain CK,Mukhopadhyay S,Ganguly A

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Esophageal cancer responds poorly to traditional therapies, and novel treatments are needed. The phytochemical curcumin is a potential treatment for Esophageal Squamous Cell Carcinoma (ESCC). A curcumin metabolite, tetrahydrocurcumin (THCUR), has anti-cancer effects and greater bioavailability than curcumin....

journal_title：Anti-cancer agents in medicinal chemistry

authors： Pendleton EG,Jamasbi RJ,Geusz ME

更新日期：2019-01-01 00:00:00