Abstract：
BACKGROUND/AIM:4H-1-Benzopyran-4-ones (chromones) provide a backbone structure for the chemical synthesis of potent anticancer drugs. In contrast to 2-(N-cyclicamino)chromones, the biological activity of 3-(N-cyclicamino)chromones has not been reported. In this study, cytotoxicity of 15 3-(N-cyclicamino)chromone derivatives was investigated and subjected to quantitative structure-activity relationship (QSAR) analysis. MATERIALS AND METHODS:Cytotoxicity against four human oral squamous cell carcinoma cell lines and three oral normal mesenchymal cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Tumor-specificity (TS) was evaluated as the ratio of mean 50% cytotoxic concentration (CC50) against normal oral cells to that against human oral squamous cell carcinoma cell lines. Potency-selectivity expression (PSE) value was calculated by dividing the TS value by the CC50 against tumor cells. Apoptosis induction was evaluated by morphological observation, western blot analysis and cell-cycle analysis. For QSAR analysis, a total of 3,096 physicochemical, structural and quantum chemical features were calculated from the most stabilized structure optimized using CORINA. RESULTS:3-(4-phenyl-1-piperazinyl)-4H-1-benzopyran-4-one (3a) had the highest tumor specificity, comparable with that of melphalan, without induction of apoptosis. Compound 3a caused cytostatic growth inhibition and had much lower cytotoxicity against human oral keratinocytes compared to doxorubicin. TS of the 15 3-(N-cyclicamino)chromones was correlated with 3D structure and lipophilicity. CONCLUSION:Chemical modification of 3a may be a potential choice for designing a new type of anticancer drug.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Shi H,Nagai J,Sakatsume T,Bandow K,Okudaira N,Uesawa Y,Sakagami H,Tomomura M,Tomomura A,Takao K,Sugita Ydoi
10.21873/anticanres.12748subject
Has Abstractpub_date
2018-08-01 00:00:00pages
4459-4467issue
8eissn
0250-7005issn
1791-7530pii
38/8/4459journal_volume
38pub_type
杂志文章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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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：1989-03-01 00:00:00
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更新日期：2015-08-01 00:00:00
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journal_title：Anticancer research
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doi：
更新日期：2002-05-01 00:00:00
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journal_title：Anticancer research
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doi：
更新日期：2000-09-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
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journal_title：Anticancer research
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doi：
更新日期：1991-09-01 00:00:00
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doi：
更新日期：2013-09-01 00:00:00
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doi：
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doi：
更新日期：2004-03-01 00:00:00
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journal_title：Anticancer research
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doi：
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1999-09-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1995-05-01 00:00:00
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journal_title：Anticancer research
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doi：
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journal_title：Anticancer research
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doi：
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doi：
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更新日期：2011-11-01 00:00:00
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doi：
更新日期：2009-08-01 00:00:00
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doi：
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journal_title：Anticancer research
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doi：
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journal_title：Anticancer research
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