Abstract：
BACKGROUND:Angiogenesis is required for tumor growth and metastasis, and is an exciting target for cancer treatment. We designed and synthesized antiangiogenetic TX agent (TX-1898, -1900), and analyzed their structural features. TXs have a chiral center and S- and R-enantiomers. Conformation analysis and molecular dynamics simulation were undertaken. MATERIALS AND METHODS:Molecular models of TXs were constructed using InsightlI-Discover. Conformation analysis was performed with CONFLEX, and z-matrix data were extracted to calculate molecular orbital (MO) parameters (i.e. solvation free energy (dGW)). Their molecular dynamics were simulated with the Discover3 module, and the total energy and dihedral angles were estimated. RESULTS:The methyl-including TXs (Group 1: TX-1863, -1878, -1866, -1879) had 130-229 conformers (-1.26-14.6 kcal/mol). The t-butyl-including group (Group 2: TX-1880, -1881, -1882, -1883) had 244 - 294 conformers (3.69 - 16. 76 kcal/mol), and the p-t-butylphenyl-containing TXs (Group 3: TX-1897, -1899, -1898, -1900) had 584 - 711 conformers (-7.48 -5.18 kcal/mol). The dGWprofile of nine samples, which were extracted from these conformers, were examined and one minimum dGW point was observed in the haloacetylcarbamoyl-2-nitroimidazole TXs (Group 1 -3). CONCLUSION:TX-1898 exhibited significant antiangiogenic activity. The order of antiangiogenic activity was as follows: TX-1898 (93% at 5 microg/pellet) > TX-1900 (82% at 5 microg/pellet) > TX-1897 (64% at 10 microg/pellet) > TX-1899 (58% at 10 microg/pellet). The chiral center has an important role for orienting the molecular characteristics.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Ohkura K,Uto Y,Nagasawa H,Hori Hsubject
Has Abstractpub_date
2007-11-01 00:00:00pages
3693-700issue
6Aeissn
0250-7005issn
1791-7530journal_volume
27pub_type
杂志文章abstract：BACKGROUND/AIM:Pancreatic neuroendocrine tumors (pNETs) are rare pancreatic neoplasms, and therapeutic options for pNETs are limited. Metformin is an anti-hypoglycemic drug that appears to have anticancer effects. However, little is known about the effect of metformin on pNETs. In this study, we investigated the anti-p...
journal_title：Anticancer research
pub_type： 杂志文章
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journal_title：Anticancer research
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journal_title：Anticancer research
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doi：
更新日期：1989-07-01 00:00:00
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journal_title：Anticancer research
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更新日期：2003-03-01 00:00:00
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更新日期：2014-05-01 00:00:00
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journal_title：Anticancer research
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pub_type： 临床试验,杂志文章,多中心研究,随机对照试验
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更新日期：2003-11-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：10.21873/anticanres.12272
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doi：
更新日期：1999-11-01 00:00:00
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journal_title：Anticancer research
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doi：
更新日期：1992-07-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2002-07-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：1994-07-01 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：
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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
pub_type： 杂志文章
doi：
更新日期：1999-01-01 00:00:00
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journal_title：Anticancer research
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doi：
更新日期：1994-03-01 00:00:00
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journal_title：Anticancer research
pub_type： 杂志文章
doi：
更新日期：2008-07-01 00:00:00
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