BORON BETAINE ANALOGS - ANTI-TUMOR ACTIVITY AND EFFECTS ON EHRLICH ASCITES TUMOR-CELL METABOLISM

被引：77

作者：

HALL, IH ^{[1
]}

STARNES, CO ^{[1
]}

SPIELVOGEL, BF ^{[1
]}

WISIANNEILSON, P ^{[1
]}

DAS, MK ^{[1
]}

WOJNOWICH, L ^{[1
]}

机构：

[1] DUKE UNIV,PAUL M GROSS CHEM LAB,DURHAM,NC 27706

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 06期

关键词：

Antineoplastic agents—betaine; boron analogs; metabolic effects; protein synthesis; nucleic acid synthesis; methyl transfer; Betaine analogs—boron; antineoplastic activity; Methylation—effect of boron betaine analogs; Nucleic acid synthesis—effect of boron betaine analogs; Protein synthesis—effect of boron betaine analogs;

D O I：

10.1002/jps.2600680607

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several newly synthesized boron betaine analogs had anti‐tumor activity in Ehrlich ascites, Walker 256 ascites carcinosarcoma, and Lewis lung screens and marginal activity in the B‐16 melanotic melanoma screen. In vivo testing demonstrated that trimethylamine‐cyanoborane inhibited Ehrlich ascites cell DNA and protein syntheses as well as gene modulation by chromatin protein phosphorylation and methylation. Trimethylamine‐cyanoborane increased cyclic‐AMP levels. In vitro testing showed that nuclear DNA polymerase, thymidylate synthetase, S‐adenosylmethyltransferase, nonhistone chromatin methylation, deoxyribonuclease, ribonuclease, and cathepsin were inhibited by the boron analogs. These compounds did not demonstrate high antitumor activity at the doses employed, but blockage of methyl transfer from S‐adenosylmethionine was established as a feasible method for controlling cell proliferation. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：685 / 688

页数：4

共 42 条

[1] COMPARISON OF SOME PROPERTIES OF AMINE-BORANES AND BORAZINES [J].