Abstract:
BACKGROUND:Sixteen 3-styryl-2H-chromenes were subjected to quantitative structure-activity relationship analysis based on their cytotoxicity, tumor selectivity and anti-HIV activity, in order to find their new biological activities. MATERIALS AND METHODS:Cytotoxicity against four human oral squamous cell carcinoma (OSCC) cell lines, three mesenchymal and two epithelial normal oral cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method. Tumor-selectivity (TS) was evaluated by the ratio of the mean CC50 (50% cytotoxic concentration) against normal human oral cells to that against OSCC cell lines. Anti-HIV activity was evaluated by the ratio of CC50 to EC50 (50% cytoprotective concentration from HIV infection). Potency-selectivity expression (PSE) was determined by the ratio of TS/CC50 against OSCC. Physicochemical, structural and quantum-chemical parameters were calculated based on the conformations optimized by the LowModeMD method. RESULTS:All 3-styryl-2H-chromene derivatives showed relatively high tumor selectivity. Especially, the compound that has a methoxy group at 7-position of the chromene ring and chlorine at 4'-position of phenyl group in styryl moiety [ 12: ] showed the highest TS and PSE values, exceeding those of resveratrol, doxorubicin and 5-FU. All compounds showed no anti-HIV activity. Among 330 chemical descriptors, 8, 74 and 16 descriptors significantly correlated to the cytotoxicity of normal and tumor cells, and tumor-specificity, respectively. CONCLUSION:Multivariate statistics with chemical descriptors for molecular shape and flatness may be useful for the evaluation of tumor-specificity of 3-styryl-2H-chromenes.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Uesawa Y,Sakagami H,Ishihara M,Kagaya H,Kanamoto T,Terakubo S,Nakashima H,Yahagi H,Takao K,Sugita Ysubject
Has Abstractpub_date
2015-10-01 00:00:00pages
5299-307issue
10eissn
0250-7005issn
1791-7530pii
35/10/5299journal_volume
35pub_type
杂志文章abstract::Urinary gonadotropin peptide (UGP) has been measured in gynecological and urological cancers, but its usefulness in the diagnosis of cancers of digestive organs has not been investigated. In this report, UGP was measured by sandwich enzyme immunoassay in 311 patients, including 166 patients with cancers of digestive o...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1996-07-01 00:00:00
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journal_title:Anticancer research
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更新日期:1992-11-01 00:00:00
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journal_title:Anticancer research
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更新日期:2014-08-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
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更新日期:2011-10-01 00:00:00
abstract::Alphafetoprotein (AFP) is an oncofetal glycoprotein that frequently reappears in sera of patients affected by hepatocellular carcinoma (HCC) and yolk-sac tumours (YST). In these cases AFP determination represents a useful marker for monitoring the therapeutic response and the clinical evolution of the neoplastic disea...
journal_title:Anticancer research
pub_type: 杂志文章,评审
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更新日期:1995-07-01 00:00:00
abstract::When mouse resident peritoneal macrophages were cultured with PSK (Krestin), a protein-bound polysaccharide extracted from Coriolus versicolor, they became enlarged and elongated and expressed higher NBT-reducing activity. PSK stimulated the production of differentiation-inducing factor and cytotoxic factor by the mou...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1991-09-01 00:00:00
abstract::Chloroethyl-nitrosourea is a potent chemotherapeutic agent for brain tumors. However, acquired resistance to this drug has become a serious problem for the treatment of patients. Previously, we established an animal model resistant to nitrosourea (Anticancer Res 19: 5313-5318, 1999). In this study, we evaluate the eff...
journal_title:Anticancer research
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doi:
更新日期:2002-07-01 00:00:00
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journal_title:Anticancer research
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更新日期:2013-03-01 00:00:00
abstract:BACKGROUND:Despite a substantial body of epidemiological evidence, there is only a limited indication that gonadotropins and steroids have growth regulating functions in ovarian cancer. To elucidate the role of gonadotropins in regulating steroid metabolism in human ovarian cancer, we analyzed the modulation of estradi...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2001-05-01 00:00:00
abstract:BACKGROUND/AIM:Identifying useful biomarkers is central to selecting optimal therapeutic strategies for esophageal squamous cell carcinoma (ESCC). Serum p53 antibody (S-p53Ab), squamous cell carcinoma antigen (SCC-Ag), and carcinoembryonic antigen (CEA) were investigated to evaluate the significance of single and combi...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.12419
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journal_title:Anticancer research
pub_type: 杂志文章,评审
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更新日期:1997-07-01 00:00:00
abstract::Vascularized bone graft (VBG) is a form of vascularized bone marrow transplant in which the bone marrow is surgically grafted with its microenvironment intact. Due to the preservation of cellular viability, VBG have significant advantages over non-vascularized bone grafts. Free vascularized fibula grafts have superior...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:2014-06-01 00:00:00
abstract:BACKGROUND/AIM:We aimed to investigate the efficacy of immune-cell therapy in terms of the survival of patients with neuroendocrine carcinoma of the uterine cervix (NECC), which lacks standardized therapeutic approaches. PATIENTS AND METHODS:We identified 17 patients who were diagnosed as having NECC and treated with ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.14475
更新日期:2020-08-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2014-05-01 00:00:00
abstract::Interleukin-2 (IL-2) has proven to be able to generate an effective anticancer immunity against both solid and hematologic malignancies. Moreover, recent advances in the knowledge of psychoneuroimmunology have demonstrated that anticancer immunity is under neuroendocrine control and that the pineal hormone melatonin (...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章
doi:
更新日期:2000-05-01 00:00:00
abstract:BACKGROUND:Prolonged exposure to asbestos, a potent carcinogen, has been the generally accepted factor responsible for the development of human mesotheliomas. Recent reports documenting the detection of SV40 DNA in human mesotheliomas suggest the possibility that this known tumor virus may be an additional factor invol...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2000-03-01 00:00:00
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doi:10.21873/anticanres.11120
更新日期:2016-10-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2015-05-01 00:00:00
abstract::In long term culture of N-ethyl-N-nitrosourea (ENU) exposed fetal BD IX-rat brains, cells proliferate and form aggregates (nodules) in vitro, starting 2-3 months after the transplacental carcinogen injection in vivo. Cell nodules of cultures from 3-6 months after ENU exposure were investigated for the presence of orga...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1984-05-01 00:00:00
abstract:BACKGROUND:Oral leukoplakia (LPL) is considered a potentially malignant disorder in the oral cavity and the gastric tract. High mobility group A (HMGA) proteins are important in the transformation of normal cells into cancer cells, but there is a lack of knowledge on their importance in oral cancer development. The aim...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2013-10-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1997-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1995-11-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,随机对照试验
doi:
更新日期:2007-01-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
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更新日期:2019-04-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2013-03-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2000-11-01 00:00:00
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更新日期:2021-01-01 00:00:00
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journal_title:Anticancer research
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doi:
更新日期:1997-01-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
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更新日期:2012-07-01 00:00:00