第二代抗耐甲氧西林金黄色葡萄球菌合成类视黄醇的构效关系及抗癌特性
Structure-Activity Relationship and Anticancer Profile of Second-Generation Anti-MRSA Synthetic Retinoids.
作者信息
Cheng Ana V, Kim Wooseong, Escobar Iliana E, Mylonakis Eleftherios, Wuest William M
机构信息
Department of Chemistry, Emory University, Atlanta, Georgia 30322 United States.
Division of Infectious Diseases, Rhode Island Hospital, Warren Alpert Medical School of Brown University, Providence, Rhode Island 02903 United States.
出版信息
ACS Med Chem Lett. 2019 Jul 17;11(3):393-397. doi: 10.1021/acsmedchemlett.9b00159. eCollection 2020 Mar 12.
Abstract
We previously reported the antibacterial activity of CD437, a known antitumor compound. It proved to be a potent antimicrobial agent effective against both growing and persister cells of methicillin-resistant (MRSA). Herein, we report the synthesis of a panel of analogs and their effect on both MRSA and cancer cells. The hydrophobic group of the parent compound was varied in steric bulk, and lipid-mimicking analogs were tested. Biological assessment confirmed that the adamantane moiety is the most effective substitution for antibacterial activity, and some preferential action in cancer over MRSA was achieved.
摘要
我们之前报道了已知抗肿瘤化合物CD437的抗菌活性。事实证明它是一种有效的抗菌剂，对耐甲氧西林金黄色葡萄球菌（MRSA）的生长细胞和持留菌均有效。在此，我们报道了一系列类似物的合成及其对MRSA和癌细胞的作用。母体化合物的疏水基团在空间体积上有所变化，并对模拟脂质的类似物进行了测试。生物学评估证实，金刚烷部分是抗菌活性最有效的取代基，并且在癌细胞中相对于MRSA实现了一些优先作用。
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