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Deletion of the C26 Methyl Substituent from the Bryostatin Analogue Merle 23 Has Negligible Impact on Its Biological Profile and Potency.
ChemBioChem ( IF 3.2 ) Pub Date : 2018-04-27 , DOI: 10.1002/cbic.201700677
Xiguang Zhao 1 , Noemi Kedei 2 , Alexandra Michalowski 2 , Nancy E Lewin 2 , Gary E Keck 1 , Peter M Blumberg 2
Affiliation  

Important strides are being made in understanding the effects of structural features of bryostatin 1, a candidate therapeutic agent for cancer and dementia, in conferring its potency toward protein kinase C and the unique spectrum of biological responses that it induces. A critical pharmacophoric element in bryostatin 1 is the secondary hydroxy group at the C26 position, with a corresponding primary hydroxy group playing an analogous role in binding of phorbol esters to protein kinase C. Herein, we describe the synthesis of a bryostatin homologue in which the C26 hydroxy group is primary, as it is in the phorbol esters, and show that its biological activity is almost indistinguishable from that of the corresponding compound with a secondary hydroxy group.

中文翻译:

从Bryostatin类似物Merle 23中删除C26甲基取代基对其生物学特性和效力的影响可忽略不计。

在理解bryostatin 1(一种癌症和痴呆症的候选治疗药物)的结构特征的作用,赋予其对蛋白激酶C的效力及其诱导的独特生物反应谱方面,正在取得重要进展。bryostatin 1中一个关键的药效团元素是C26位置的仲羟基,相应的伯羟基在佛波酯与蛋白激酶C的结合中起类似作用。在此,我们描述了bryostatin同源物的合成C26羟基是佛波酯中的伯羟基,表明其生物学活性与带有仲羟基的相应化合物的生物学活性几乎没有区别。
更新日期:2018-04-27
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