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首页> 外文期刊>RSC Advances >New dihydropyrimidin-2(1H)-one based Hsp90 C-terminal inhibitors
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New dihydropyrimidin-2(1H)-one based Hsp90 C-terminal inhibitors

机译：新的基于二氢嘧啶-2（1H）-one的Hsp90 C末端抑制剂

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The inhibition of the C-terminal domain of heat shock protein 90 (Hsp90) is emerging as a novel strategy for cancer therapy, therefore the identification of a new class of C-terminal inhibitors is strongly required, also in consideration that to date only nature-inspired molecules have been largely expanded. Our recent discovery of potent antiproliferative dihydropyrimidone based C-terminal Hsp90 inhibitor (1, IC50 = 50.8 +/- 0.2 mu M and 20.8 +/- 0.3 mu M in A375 and Jurkat cell lines, respectively) drove us to further explore this very promising pharmacophoric core. In this study, we identified a new set of DHPM-derivatives that exhibited antiproliferative activity against two cancer lines by their modulation of Hsp90 C-terminus without inducing the undesired heat shock response. Our results strongly outline the high sensitivity of the Biginelli scaffold to structural decorations allowing us to point out also that small variations can deeply influence biological activity.
机译：抑制热休克蛋白90（Hsp90）的C端结构域已成为一种新的癌症治疗策略，因此，强烈考虑到迄今为止，仅出于性质考虑，就需要鉴定一类新的C端抑制剂受启发的分子已大大扩展。我们最近发现的基于强效抗增殖二氢嘧啶酮的C端Hsp90抑制剂（分别在A375和Jurkat细胞系中的IC50 = 50.8 +/- 0.2μM和20.8 +/- 0.3μM）使我们进一步探索这一非常有希望的药效团核心。在这项研究中，我们确定了一套新的DHPM衍生物，它们通过调节Hsp90 C末端而对两个癌症系表现出抗增殖活性，而不会引起不希望的热激反应。我们的结果强烈概述了Biginelli支架对结构装饰的高度敏感性，这使我们也指出，小的变化会深刻影响生物活性。

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