Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors

Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors
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DOI:
10.1016/j.bmcl.2011.10.011
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发表时间:
2011-12-15
影响因子:
2.7
通讯作者:
Fahl, William E.
Fahl, William E.
中科院分区:
医学4区
文献类型:
--
作者:
Copp, Richard R.;Peebles, Daniel D.;Fahl, William E.

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报道了 PrC-210 氨基硫醇、3-(甲基氨基)-2-((甲基氨基)甲基)丙烷-1-硫醇及其多胺和硫醇化多胺祖细胞的合成、生长抑制和辐射防护活性。所有分子均显着抑制培养的正常人成纤维细胞的生长。 ROS清除硫醇基团和带正电荷的烷基胺主链的组合提供了最具辐射防护性的氨基硫醇分子。 (C) 2011 Elsevier Ltd. 保留所有权利。
The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methylamino)-2-((methylamino) methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule. (C) 2011 Elsevier Ltd. All rights reserved.