Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs.

Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs.
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同基噻唑啉 - 恶唑类似物的合成和HDAC抑制活性。

DOI:
10.1016/j.bmcl.2013.06.012
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发表时间:
2013-11-01
影响因子:
2.7
通讯作者:
Williams, Robert M.
Williams, Robert M.
中科院分区:
医学4区
文献类型:
--
作者:
Guerra-Bubb, Jennifer M.;Bowers, Albert A.;Smith, William B.;Paranal, Ronald;Estiu, Guillermina;Wiest, Olaf;Bradner, James E.;Williams, Robert M.

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描述了天然产物和HDAC抑制剂largazole的电子等排类似物的合成。天然产物噻唑环中的硫原子被氧原子取代,构成恶唑环。描述了该物种的生物化学活性和细胞毒性。
The synthesis of an isosteric analog of the natural product and HDAC inhibitor largazole is described. The sulfur atom in the thizaole ring of the natural product has been replaced with an oxygen atom, constituting an oxazole ring. The biochemical activity and cytotoxicity of this species is described.
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