Pilot in Vivo Structure–Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O6-Methylguanine and Lung Tumor in A/J Mice,Journal of Medicinal Chemistry

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Pilot in Vivo Structure–Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O6-Methylguanine and Lung Tumor in A/J Mice
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-09-13 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00921
Manohar Puppala ₁ , Sreekanth C. Narayanapillai _{1,

2} , Pablo Leitzman ₁ , Haifeng Sun ₂ , Pramod Upadhyaya ₃ , M. Gerard O’Sullivan _{4,

5} , Stephen S. Hecht ₃ , Chengguo Xing _{1,

2}

Affiliation

(+)-Dihydromethysticin was recently identified as a promising lung cancer chemopreventive agent, while (+)-dihydrokavain was completely ineffective. A pilot in vivo structure–activity relationship (SAR) was explored, evaluating the efficacy of its analogs in blocking 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced short-term O⁶-methylguanine and long-term adenoma formation in the lung tissues in A/J mice. Both results revealed cohesive SARs, demonstrating that the methylenedioxy functional group in DHM is essential while the lactone functional group tolerates modifications.

中文翻译：

体内结构的试验-二氢甲基美天青素在A / J小鼠中阻断4-（甲基亚硝胺基）-1-（3-吡啶基）-1-丁酮诱导的O ^6-甲基鸟嘌呤和肺肿瘤的活性关系

（+）-二氢甲氧苄啶最近被确定为一种有前途的肺癌化学预防剂，而（+）-二氢卡伐他汀则完全无效。探索了体内结构-活性关系的初步试验，评估了其类似物在阻断4-（甲基亚硝胺基）-1-（3-吡啶基）-1-丁酮诱导的短期O ^6-甲基鸟嘌呤和长效中的功效。A / J小鼠肺组织中的长期腺瘤形成。两项结果均显示出内聚性SAR，表明DHM中的亚甲二氧基官能团是必不可少的，而内酯官能团则可耐受修饰。

更新日期：2017-09-13

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