Synthesis of Naphthoic Acids as Potential Anticancer Agents,Synlett

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Synthesis of Naphthoic Acids as Potential Anticancer Agents
Synlett ( IF 1.7 ) Pub Date : 2018-12-03 , DOI: 10.1055/s-0037-1611342
Lorraine Deck ₁ , Jacob Greenberg ₁ , Lisa Whalen ₁ , David Vander Jagt ₂ , Robert Royer ₂

Affiliation

As part of ongoing research to investigate structural requirements for lactate dehydrogenase inhibition by highly substituted naphthoic acids, nine new aryl-substituted dihydroxynaphthoic acids were synthesized from three known precursors. Described here are efficient preparations of the 1-naphthoic acid target compounds by using Suzuki coupling reactions, formylations, oxidations, and demethylations. Lactate dehydrogenase inhibition studies conducted with five of the compounds revealed values of the inhibitory constant K i in the low micromolar range.

中文翻译：

作为潜在抗癌剂的萘甲酸的合成

作为研究高度取代的萘甲酸对乳酸脱氢酶抑制的结构要求的持续研究的一部分，从三种已知的前体合成了九种新的芳基取代的二羟基萘甲酸。这里描述的是通过使用 Suzuki 偶联反应、甲酰化、氧化和去甲基化有效制备 1-萘甲酸目标化合物。用五种化合物进行的乳酸脱氢酶抑制研究揭示了低微摩尔范围内的抑制常数 K i 值。

更新日期：2018-12-03

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