2010 Fiscal Year Final Research Report
Development of low toxicity topoisomerase inhibitor (anticancer medicine) with treatment and protective efficacy
| Project/Area Number |
20590109
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Yokohama College of Pharmacy |
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Principal Investigator |
SUZUKI Keitarou Yokohama College of Pharmacy, 薬学部, 教授 (10154535)
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| Co-Investigator(Kenkyū-buntansha) |
HOSONO Tetsuji 横浜薬科大学, 薬学部, 講師 (20450554)
OMATA Yoshiaki 横浜薬科大学, 薬学部, 教授 (20268840)
OOKAWARA Tadashi 熊本保健科学大学, 保健科学部, 教授 (60040325)
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| Project Period (FY) |
2008 – 2010
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| Keywords | 生物活性物質 / 抗がん薬 / トポイソメラーゼ / 酵素阻害 |
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| Research Abstract |
Tris(galloylamino)benzene (TGBA) derivatives were prepared and their inhibitory activities were measured against human topoisomerase (topo) I and II. TGBA derivatives with many OH group showed strong inhibition against the topo I and II. Unlike camptothecin and etoposide which are the inhibitors, TGBA derivatives directly inhibited the activities of topo I and II in earlier step than the formation of topo-DNA complex, which did not stabilized DNA-topo cleavable complex. In anti cancer effects for various cancer cell lines, TGBA derivatives showed the inhibitory effects of cell growth for brain and lung cancer cell lines. These results suggests that TGBA derivatives are an anticancer drug by topo inhibition of a new type, and could be candidates as lead compounds of anti-brain and anti-lung cancer drugs.
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