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ET-18-OCH3的环状醚类似物SRI 62-834的抗肿瘤活性

Antitumor activity of SRI 62-834, a cyclic ether analog of ET-18-OCH3.

作者信息

Houlihan W J, Lee M L, Munder P G, Nemecek G M, Handley D A, Winslow C M, Happy J, Jaeggi C

机构信息

Sandoz Research Institute, East Hanover, New Jersey 07936.

出版信息

Lipids. 1987 Nov;22(11):884-90. doi: 10.1007/BF02535549.

Abstract

SRI 62-834, an analog of the antitumor agent ET-18-OCH3 in which the oxygen atom at carbon atom 2 has been incorporated into a five-membered heterocycle, has been prepared and evaluated as an antitumor agent. The compound exhibited good cytotoxicity in vitro against a variety of tumor cell lines and was as effective as ET-18-OCH3 given orally in the mouse Meth A sarcoma model. SRI 62-834 was shown to be an inhibitor of platelet-derived growth factor (PDGF), possibly at the receptor level, and platelet-activating factor (PAF) at the receptor level.

摘要

SRI 62 - 834是抗肿瘤药物ET - 18 - OCH3的类似物,其中碳原子2上的氧原子已被并入一个五元杂环中,该化合物已被制备并作为抗肿瘤药物进行评估。该化合物在体外对多种肿瘤细胞系表现出良好的细胞毒性,并且在小鼠Meth A肉瘤模型中口服给药时与ET - 18 - OCH3效果相当。SRI 62 - 834被证明是血小板衍生生长因子(PDGF)的抑制剂,可能作用于受体水平,同时也是受体水平的血小板活化因子(PAF)的抑制剂。

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