Abstract：
:The melanin biosynthetic pathway from tyrosine is a potential target for combating malignant melanoma. N-Acetyl-4-S-cysteaminylphenol 1 is a previously synthesized analogue of tyrosine that probably acts by this pathway. It interferes with cell growth and proliferation via selective oxidation in melanocytes to an oquinone that can alkylate cellular nucleophiles. We previously synthesized a range of analogues of the original lead compound 1 most of which displayed greater cytotoxicity than 1. Eighteen new analogues with the amide group reversed have now been synthesized and tested for antimelanoma activity. Most of these reverse amides showed greater cytotoxicity than N-acetyl-4-S-cysteaminylphenol towards five representative melanoma cell lines. The highest cytotoxicity was observed for the piperidine and hexamethyleneimine derivatives 7, 8, 12, 13, and 17 and the catechol 18. The most active compound, 7, had cytotoxicity comparable to cisplatin against the five melanoma cell lines. The moderate activity of 7 and 18 against SK-Mel-24 (non-tyrosinase containing) and an ovarian cell line suggests that interference with the melanin pathway may not be the only mode of action of these compounds. Assays of some of the compounds as substrates for tyrosinase showed that the catechol 18 was the best substrate and that the piperidine derivative 7 was the best substrate of the phenolic compounds synthesized.
journal_name
Oncol Resjournal_title
Oncology researchauthors
Nicoll K,Robertson J,Lant N,Kelland LR,Rogers PM,Robins DJdoi
10.3727/000000006783981206subject
Has Abstractpub_date
2006-01-01 00:00:00pages
97-106issue
2eissn
0965-0407issn
1555-3906journal_volume
16pub_type
杂志文章abstract：:Although epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) are used as first-line agents for treating nonsquamous cell lung cancer with EGFR mutation, there are many patients who have to receive these drugs following platinum-based chemotherapy. This study was designed to define whether exposure ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504012x13285365944337
更新日期：2011-01-01 00:00:00
abstract：: THIS ARTICLE WAS WITHDRAWN BY THE PUBLISHER IN NOVEMBER 2020. ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504018X15165493852990
更新日期：2018-10-17 00:00:00
abstract：:To ascertain whether insulin-like growth factors (IGF-1 and IGF-2) affect the estrogen- and insulin-responsive R3230AC mammary carcinoma, studies of IGF-1 and IGF-2 receptors were conducted on primary-culture tumor cells and on membranes purified from whole tumors. By saturation binding analysis, cells in culture disp...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1992-01-01 00:00:00
abstract：:Hepatocellular carcinoma (HCC) is a disease with poor prognosis rates and ineffective therapeutic options. Previous studies have reported the involvement of mitogen-inducible gene 6 (MIG-6) as a negative regulator in tumor formation. MicroRNAs (miRNAs) play crucial roles in the development of different types of cancer...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X15000784459799
更新日期：2018-05-07 00:00:00
abstract：:The human nucleolar protein p120 is highly expressed in human cancers. Its high expression in breast cancer correlates with a poor prognosis, and its overexpression in 3T3 mouse fibroblasts causes malignant transformation. This study reports that a combination of monoclonal anti-p 120 antibody (MAbp120), liposomes (Li...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1996-01-01 00:00:00
abstract：:Ahead of Print article withdrawn by publisher. ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504016X14747357310629
更新日期：2016-09-30 00:00:00
abstract：:Topotecan, a topoisomerase I poison and water-soluble derivative of camptothecin, has shown promise in treating solid tumors; however, the drug is unstable under physiological conditions and converts to an inactive form within 30 minutes. Encapsulating topotecan in liposomes (LIP-TPT) minimizes inactivation. The effic...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1995-01-01 00:00:00
abstract：:We previously reported that 9-methylstreptimidone, a piperidine compound isolated from a culture filtrate of Streptomyces, induces apoptosis selectively in adult T-cell leukemia cells. It was screened for a compound that inhibits LPS-induced NF-kappaB and NO production in mouse macrophages. However, 9-methystreptimido...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504012x13425470196056
更新日期：2012-01-01 00:00:00
abstract：:We previously reported that vasoactive intestinal polypeptide (VIP) significantly inhibited Matrigel invasion and haptotactic migration of murine colon 26-L5 carcinoma in vitro. To extend our study, we investigated the inhibitory mechanisms of VIP on Matrigel invasion of colon 26-L5 carcinoma, and the effect on metast...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1998-01-01 00:00:00
abstract：:Empty spiracles homeobox 2 (EMX2) is a homeodomain-containing transcription factor that plays an essential role in tumorigenesis. However, to the best of our knowledge, the role of EMX2 in human colorectal cancer (CRC) is still unclear. Thus, the aim of this study was to investigate the expression and role of EMX2 in ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504016X14756640150695
更新日期：2017-04-14 00:00:00
abstract：:The potency of flavonoids (isoflavones, flavones, and flavanones) to inhibit efflux of 2',7'-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) from human erythrocytes was investigated. Structure-activity relationship analysis showed that the strongest inhibitors were found among flavanones bearing a hydrophobic pren...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/000000003108747983
更新日期：2003-01-01 00:00:00
abstract：:The aim of this study was to analyze the efficacy according to EGFR status and predictors of TKIs in Chinese advanced lung adenocarcinoma patients in a single institute. We retrospectively enrolled 253 patients with advanced or recurrent adenocarcinoma and history of EGFR-TKI treatment attended at Beijing Chest Hospit...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504014X13907540404833
更新日期：2014-01-01 00:00:00
abstract：:Medullary thyroid carcinoma (MTC) is an uncommon and highly aggressive tumor of the neuroendocrine system, which derives from the neuroendocrine C cells of the thyroid gland. Except for surgical resection, there are not very many effective systemic treatment options for MTC. N-Myc downstream-regulated gene 2 (NDRG2) h...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504015X14452563486093
更新日期：2016-01-01 00:00:00
abstract：:The pre-mRNA splicing regulator serine-arginine protein kinase 1 (SRPK1), a member of the SR kinase family, plays an essential role in cancer development and various pathophysiological processes. However, its expression pattern and functions in renal cell carcinoma (RCC) remain unknown. Therefore, the aim of this stud...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504016X14743324568129
更新日期：2017-03-13 00:00:00
abstract：:The ability of mitoxantrone to form DNA adducts was investigated in a series of human tumor cell lines consisting of human cervical cancer (HeLa), human breast cancer (MCF-7), and human neuroblastoma (IMR-32) cells. The mitoxantrone-resistant human promyelocytic leukemia cell line HL60/MX2 was also compared to the par...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504003773994815
更新日期：2004-01-01 00:00:00
abstract：:Heme oxygenase-1 (HO-1) plays an important role in the progression of several malignancies including breast cancer. However, its role in breast cancer metastasis is still ambiguous. In this study, we observed the effect of HO-1 on mouse mammary carcinoma metastasis using the in vivo tumor metastasis model. Our results...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504018X15415906335771
更新日期：2019-06-21 00:00:00
abstract：:Treatment of female SKH-1 hairless mice with ultraviolet B light twice a week for 20 weeks resulted in a population of tumor-free mice with a high risk of developing skin tumors during the next several months in the absence of additional UVB treatment (high-risk mice). Topical applications of nondenatured soymilk but ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/0965040041292350
更新日期：2004-01-01 00:00:00
abstract：:HeLa cells were transfected with full-length multidrug resistance protein (MRP) cDNA and with MRP cDNAs that had been mutated at certain nucleotide binding domains. Stable transfectants were isolated and those producing equivalent amounts of P190 were tested in cytotoxicity assays using a variety of chemotherapeutic a...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1997-01-01 00:00:00
abstract：:The potential of American ginseng (AG) ( Panax quinquefolium), a commonly used herbal remedy believed to have anticarcinogenic effects, to prevent the development of mammary tumors was evaluated in a mouse model of dimethylbenzanthracene (DMBA)-induced mammary carcinoma. Ginsenosides, believed to be the active compone...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/000000006783981017
更新日期：2006-01-01 00:00:00
abstract：:A series of bis-aziridinylnaphthoquinone derivatives has been prepared. The cytotoxic activities and DNA alkylation abilities of these synthetic bis-aziridinylnaphthoquinone derivatives were investigated. They displayed significant cytotoxicity against human carcinomna cell lines and weak cytotoxic activities against ...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：2003-01-01 00:00:00
abstract：:Head and neck squamous cell carcinoma (HNSCC) ranks as the sixth most frequent cancer worldwide. HNSCC cell lines are typically refractory to transforming growth factor-beta (TGF-beta)-mediated cell cycle arrest. A number of these cell lines carry inactivating mutations of the TGF-beta type II (TbetaR-II) receptor, an...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/000000003108748612
更新日期：2003-01-01 00:00:00
abstract：:Recently, there has been significant effort in developing techniques designed to detect disseminated tumor cells in the peripheral blood (PB). These techniques include immunocytochemical staining of cytocentrifuge slides, flow cytometry, and RT-PCR. Several authors reported various results concerning the sensitivity o...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1999-01-01 00:00:00
abstract：:Gastric cancer (GC) is the most common epithelial malignancy worldwide. Basic transcription factor 3 (BTF3) plays a crucial role in the regulation of various biological processes. We designed experiments to investigate the molecular mechanism underlying the role of BTF3 in GC cell proliferation and metastasis. We conf...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X14886494526344
更新日期：2017-11-02 00:00:00
abstract：:This study was designed to investigate the role of miR-183 in modulating cell growth and apoptosis of tongue squamous cell carcinoma SCC25 cell line. Human squamous epithelial cell and squamous cell carcinoma cell line SCC25 was used, and miR-183 was inhibited. Cell growth, colony formation, and apoptotic rate, as wel...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504016X14685034103239
更新日期：2016-10-27 00:00:00
abstract：:Laryngeal cancer, one of the most common head and neck malignancies, is an aggressive neoplasm. Increasing evidence has demonstrated that microRNAs (miRNAs) exert important roles in oncogenesis and progression of diverse types of human cancers. miR-632, a tumor-related miRNA, has been reported to be dysregulated and i...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504018X15213142076069
更新日期：2020-02-07 00:00:00
abstract：:There is growing evidence on the clinical significance of Tumor Microenvironment (TME) cells in predicting prognosis and therapeutic effects. However, cell interactionsin tumor microenvironments have not been thoroughly studied or systematicallyanalyzed so far. In this study, 22 immune cell components in the lung aden...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504020X15907428281601
更新日期：2020-05-29 00:00:00
abstract：:The effects of treatment of HeLa cells with the antitumor nucleoside analog 2'-deoxy-2'-(fluoromethylene) cytidine (FMdC) on ultraviolet and X-ray sensitivity were examined. A 1-h pretreatment with FMdC increased cellular sensitivity to both X-rays and ultraviolet irradiation as determined by survival curve analysis. ...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1994-01-01 00:00:00
abstract：:In colorectal cancers, the local cytokine network and the levels of nitric oxide (NO) and reactive oxygen species (ROS) are known to be closely related to cancer progression and metastasis, but the influence of the currently administered therapies on the cancer microenvironment is not completely understood. We analyze...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504010x12671222663593
更新日期：2010-01-01 00:00:00
abstract：:Human glioblastoma multiforme (GBM) accounts for the majority of human brain gliomas. Several TMEM proteins, such as TMEM 45A, TMEM 97, and TMEM 140, are implicated in human brain gliomas. However, the roles of TMEM168 in human GBM remain poorly understood. Herein we found that mRNA levels of TMEM168 were overexpresse...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504018X15478559215014
更新日期：2019-07-12 00:00:00
abstract：:Our recent studies have shown that vanadium, a dietary micronutrient, has an inhibitory response against experimentally induced rat liver carcinogenesis. In the present study, the effect of vanadium on hepatic xenobiotic biotransformation in rats exposed to diethylnitrosamine (DENA, 200 mg/kg, IP) was investigated to ...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1999-01-01 00:00:00
