Synthesis of quinazolines as tyrosine kinase inhibitors.

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: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：:Recently mutual interactions of chemotherapy and immunotherapy have been widely accepted, and several synergistic mechanisms have been elucidated as well. Although much attention has focused on the combination of DC vaccine and chemotherapy, there are still many problems remaining to be resolved, including the optimal...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Dong W,Wei R,Shen H,Ni Y,Meng L,Du J

更新日期：2016-01-01 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：: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：INTRODUCTION:Inflammation is a vital reaction of the natural immune system that protects against encroaching agents. However, uncontrolled inflammation can lead to complications. Trigonella foenum-graecum is traditionally used as an anti-inflammatory herb. OBJECTIVES:The current study was conducted to explore the anti...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Asif M,Yousaf HM,Saleem M,Saadullah M,Chohan TA,Shamas MU,Yaseen HS,Mahrukh,Yousaf MU,Yaseen M

更新日期：2020-10-04 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：BACKGROUND AND OBJECTIVE:Glucosamine is a widely prescribed dietary supplement used in the treatment of osteoarthritis. In the present study, the chemoprotectant ability of glucosamine was evaluated against cisplatin-induced genotoxicity and cytotoxicity in rat bone marrow cells. METHODS:Glucosamine was orally adminis...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Cheki M,Jafari S,Najafi M,Mahmoudzadeh A

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Hepatocellular Carcinoma (HCC), the second leading cause of cancer-related mortality with over half a million new cases diagnosed annually in the world, accounts for nearly 70% of cancer deaths in parts of Asia and Africa. Podophyllum, one of the important members of the lignane class of natural products der...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Chen H,Zhang M,Wang Z,Li L,Li Q,Wang H

更新日期：2020-01-01 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：:Mammalian target of rapamycin (mTOR) is a central controller of cell growth, proliferation, metabolism and angiogenesis. mTOR signaling is often dysregulated in various human diseases and thus attracts great interest in developing drugs that target mTOR. Currently it is known that mTOR functions as two complexes, mTOR...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Zhou H,Luo Y,Huang S

更新日期：2010-09-01 00:00:00

abstract：BACKGROUND:High-risk human papillomavirus (HR-HPV) persistent infection is the main cause of cervical cancer and its precancerous lesions. A previous study showed that HPV16 and HPV58 infections were the most common infection types in the local region. Some studies also declared that HPV58 E7 variants increased the ris...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Tian S,Zhang L,Li Y,Cao D,Quan S,Guo Y,Yang X,Yang T

更新日期：2020-11-05 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：: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：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 favorab...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Detroja D,Chen TL,Lin YW,Yen TY,Wu MH,Tsai TH,Mehariya K,Kakadiya R,Lee TC,Shah A,Su TL

更新日期：2017-01-01 00:00:00

abstract：:Cilengitide, a cyclic RGD pentapeptide, is currently in clinical phase III for treatment of glioblastomas and in phase II for several other tumors. This drug is the first anti-angiogenic small molecule targeting the integrins αvβ3, αvβ5 and αvβ1. It was developed by us in the early 90s by a novel procedure, the spatia...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Mas-Moruno C,Rechenmacher F,Kessler H

更新日期：2010-12-01 00:00:00

abstract：:A majority of breast cancers (BC) display characteristics of epithelial cells and express estrogen receptors and/or HER-2 (a member of the epidermal growth factor receptor family). About one-fifth of BC is constituted of basal cells for which there is no specific category of proliferation regulators. Insulin-like grow...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Mester J,Redeuilh G

更新日期：2008-12-01 00:00:00

abstract：:The rapid approval of several novel agents has given prostate cancer patients and their treating physicians many new and effective therapeutic options. Four new medical therapies were recently approved on the basis of prolonged overall survival in castration-resistant prostate cancer (CRPC) patients: sipuleucel-T, cab...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Massari F,Maines F,Modena A,Brunelli M,Bria E,Artibani W,Martignoni G,Tortora G

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND:Sonchus oleraceus is a large and widespread plant in the world. It is edible to humans as a leaf vegetable and is also used as a folklore medicinal herb in the treatment of infections and inflammatory disease, but limited research on its chemical constituents has been done. OBJECTIVE:To isolate and identify...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Zhang H,Wang Y,Wang S,Wang Q,Wang T,Zhu J,Liu B

更新日期：2020-01-01 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：:Classical chemotherapeutic agents such as mitotic inhibitors (spindle poisons), alkylating agents, antimetabolites, topoisomerase inhibitors, and anthracenediones (anthracyclines) inhibit DNA synthesis and mitosis, thereby killing or impeding the proliferation of rapidly dividing cells. During the last decade, targete...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Kontos CK,Christodoulou MI,Scorilas A

更新日期：2014-03-01 00:00:00

abstract：BACKGROUND:Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor that regulates the expression of many genes relevant to carcinogenesis. By analogy to selective estrogen receptor modulator for treatment of cancer, selective or partial PPARγ agonists are considered clinically important for chemo...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Joshi H,Marulkar K,Gota V,Ramaa CS

更新日期：2017-01-01 00:00:00

abstract：:Colorectal cancer is a major global health problem with more than a million new cases diagnosed worldwide in 2005. In the United States, this malignancy is the third most common with 145,000 new cases and the second most lethal with 56,000 deaths in 2005. Unfortunately, preclinical diagnostic screening in the U.S. pop...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Majer M,Akerley W,Kuwada SK

更新日期：2007-09-01 00:00:00

abstract：AIM:The aim of this study is to explore the therapeutic potential of S-allylcysteine (SAC) organosulphur compound as potent immune checkpoint inhibitor PD-L1. BACKGROUND:Natural compounds have been showing tremendous anticancerous potential via suppressing the expression of genes involved in development and progressio...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Khan F,Pandey P,Mishra R,Arif M,Kumar A,Jafri A,Mazumder R

更新日期：2020-07-28 00:00:00

abstract：:Glioblastoma Multiforme (GMB) is the most aggressive primary brain tumor with poor survival rates and universal recurrence despite aggressive treatments. Recent research suggested that GBM has multiple glioma cell populations, some of which are organized in a stem cell hierarchical order with different stages of diffe...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Alexandru-Abrams D,Jadus MR,Hsu FP,Stathopoulos A,Bota DA

更新日期：2014-01-01 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：BACKGROUND:Reserpine, an indole alkaloid commonly used for hypertension, is found in the roots of Rauwolfia serpentina. Although the root extract has been used for the treatment of cancer, the molecular mechanism of its anti-cancer activity on hormonal independent prostate cancer remains elusive. METHODS:we evaluated ...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Ramamoorthy MD,Kumar A,Ayyavu M,Dhiraviam KN

更新日期：2018-01-01 00:00:00

abstract：:The hypothesis that vitamin D deficiency increases the risk of clinical prostate cancer has stimulated an extensive body of research. Ecologic studies have shown that mortality rates from prostate cancer are inversely correlated with levels of ultraviolet radiation, the principal source of vitamin D. Human prostate ce...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Schwartz GG

更新日期：2013-01-01 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：:The sequence specificity of the anti-tumour drug, cisplatin, was determined in a DNA sequence that contained seven telomeric repeats and a run of ten consecutive guanine bases. Cisplatin preferentially forms DNA adducts at consecutive guanine sequences. Hence these DNA sequences were examined in order to gain an insig...

journal_title：Anti-cancer agents in medicinal chemistry

authors： Murray V,Kandasamy N

更新日期：2012-03-01 00:00:00