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烟曲霉素的化学修饰。I. 6-O-酰基、6-O-磺酰基、6-O-烷基和6-O-(N-取代氨基甲酰基)烟曲霉素醇

Chemical modification of fumagillin. I. 6-O-acyl, 6-O-sulfonyl, 6-O-alkyl, and 6-O-(N-substituted-carbamoyl)fumagillols.

作者信息

Marui S, Itoh F, Kozai Y, Sudo K, Kishimoto S

机构信息

Chemistry Research Laboratories, Takeda Chemical Industries, Ltd., Osaka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Jan;40(1):96-101. doi: 10.1248/cpb.40.96.

DOI:10.1248/cpb.40.96
PMID:1374294
Abstract

The hydroxy group of fumagillol (3), a degradation product of fumagillin (1), was acylated, sulfonylated, alkylated or carbamoylated, and the anti-angiogenic activity of the resulting products was examined. These compounds inhibited the angiogenesis induced by basic fibroblast growth factor in the rat corneal micropocket assay and the growth of vascular endothelial cells in vitro. Among them, compound 2 (AGM-1470) was found to show the most potent inhibitory effect on the growth of vascular endothelial cells and was selected from this series as a candidate for further development.

摘要

烟曲霉素（1）的降解产物烟曲霉素醇（3）的羟基被酰化、磺酰化、烷基化或氨甲酰化，并检测了所得产物的抗血管生成活性。这些化合物在大鼠角膜微袋试验中抑制了碱性成纤维细胞生长因子诱导的血管生成以及体外血管内皮细胞的生长。其中，化合物2（AGM - 1470）对血管内皮细胞的生长显示出最有效的抑制作用，并从该系列中被选作进一步开发的候选物。

相似文献

1
Chemical modification of fumagillin. I. 6-O-acyl, 6-O-sulfonyl, 6-O-alkyl, and 6-O-(N-substituted-carbamoyl)fumagillols.烟曲霉素的化学修饰。I. 6-O-酰基、6-O-磺酰基、6-O-烷基和6-O-(N-取代氨基甲酰基)烟曲霉素醇
Chem Pharm Bull (Tokyo). 1992 Jan;40(1):96-101. doi: 10.1248/cpb.40.96.
2
Potent anti-angiogenic action of AGM-1470: comparison to the fumagillin parent.AGM-1470的强效抗血管生成作用：与烟曲霉素母体的比较。
Biochem Biophys Res Commun. 1991 Feb 14;174(3):1070-6. doi: 10.1016/0006-291x(91)91529-l.
3
Frequent administration of angiogenesis inhibitor TNP-470 (AGM-1470) at an optimal biological dose inhibits tumor growth and metastasis of metastatic human transitional cell carcinoma in the urinary bladder.以最佳生物学剂量频繁给予血管生成抑制剂TNP - 470（AGM - 1470）可抑制人膀胱转移性移行细胞癌的肿瘤生长和转移。
Clin Cancer Res. 2002 Jul;8(7):2389-98.
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Simulation of human B-lymphocyte proliferation by AGM-1470, a potent inhibitor of angiogenesis.血管生成强效抑制剂AGM - 1470对人B淋巴细胞增殖的模拟作用
J Natl Cancer Inst. 1995 Jan 18;87(2):136-9. doi: 10.1093/jnci/87.2.136.
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The rat Subcutaneous Air Sac model: a quantitative assay of antiangiogenesis in induced vessels.大鼠皮下气囊模型：诱导血管中抗血管生成的定量测定
Pharmacol Toxicol. 1999 Jan;84(1):34-40. doi: 10.1111/j.1600-0773.1999.tb02108.x.
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Effects of AGM-1470 and pentosan polysulphate on tumorigenicity and metastasis of FGF-transfected MCF-7 cells.AGM - 1470和戊聚糖多硫酸酯对成纤维细胞生长因子转染的MCF - 7细胞致瘤性和转移的影响。
Br J Cancer. 1996 May;73(9):1053-62. doi: 10.1038/bjc.1996.204.
7
Inhibition of tumor growth and metastasis of rodent tumors by the angiogenesis inhibitor O-(chloroacetyl-carbamoyl)fumagillol (TNP-470; AGM-1470).血管生成抑制剂O-(氯乙酰-氨甲酰基)烟曲霉素(TNP-470；AGM-1470)对啮齿类动物肿瘤生长和转移的抑制作用
Cancer Res. 1993 Sep 15;53(18):4262-7.
8
Investigation of novel fumagillin analogues as angiogenesis inhibitors.
Bioorg Med Chem Lett. 2004 Jan 5;14(1):91-4. doi: 10.1016/j.bmcl.2003.10.008.
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The role of angiogenesis in the tumor growth of Syrian hamster pancreatic cancer cell line HPD-NR.血管生成在叙利亚仓鼠胰腺癌细胞系HPD-NR肿瘤生长中的作用。
Gastroenterology. 1995 May;108(5):1526-33. doi: 10.1016/0016-5085(95)90703-3.
10
In vitro inhibition of endothelial cell growth by the antiangiogenic drug AGM-1470 (TNP-470) and the anti-endoglin antibody TEC-11.抗血管生成药物AGM - 1470（TNP - 470）和抗内皮糖蛋白抗体TEC - 11对内皮细胞生长的体外抑制作用。
Anticancer Drugs. 1997 Mar;8(3):238-44. doi: 10.1097/00001813-199703000-00004.

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Common therapeutic target for both cancer and obesity.癌症和肥胖症的共同治疗靶点。
World J Biol Chem. 2017 May 26;8(2):102-107. doi: 10.4331/wjbc.v8.i2.102.
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Orally active fumagillin analogues: transformations of a reactive warhead in the gastric environment.口服活性烟曲霉素类似物：反应弹头在胃部环境中的转化
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The antiangiogenic agent TNP-470 requires p53 and p21CIP/WAF for endothelial cell growth arrest.抗血管生成剂TNP - 470使内皮细胞生长停滞需要p53和p21CIP/WAF。
Proc Natl Acad Sci U S A. 2000 Nov 7;97(23):12782-7. doi: 10.1073/pnas.97.23.12782.
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Inhibition of growth and metastasis of ovarian carcinoma by administering a drug capable of interfering with vascular endothelial growth factor activity.通过给予一种能够干扰血管内皮生长因子活性的药物来抑制卵巢癌的生长和转移。
Jpn J Cancer Res. 1996 Sep;87(9):963-71. doi: 10.1111/j.1349-7006.1996.tb02127.x.
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Cytostatic inhibition of endothelial cell growth by the angiogenesis inhibitor TNP-470 (AGM-1470).血管生成抑制剂TNP - 470（AGM - 1470）对内皮细胞生长的细胞生长抑制作用
Br J Cancer. 1994 Feb;69(2):212-6. doi: 10.1038/bjc.1994.41.
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Anti-proliferative effects of TNP-470 on human malignant glioma in vivo: potent inhibition of tumor angiogenesis.TNP-470对人恶性胶质瘤的体内抗增殖作用：对肿瘤血管生成的有效抑制
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J Neurooncol. 1995;23(1):23-9. doi: 10.1007/BF01058456.
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Antitumor effect of arterial administration of a medium-chain triglyceride solution of an angiogenesis inhibitor, TNP-470, in rabbits bearing VX-2 carcinoma.血管生成抑制剂TNP - 470的中链甘油三酯溶液动脉给药对荷VX - 2癌兔的抗肿瘤作用
Pharm Res. 1995 May;12(5):653-7. doi: 10.1023/a:1016243105622.