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

Manohar Puppala, Sreekanth C. Narayanapillai, Pablo Leitzman, Haifeng Sun, Pramod Upadhyaya, M. Gerard O'Sullivan, Stephen S. Hecht, Chengguo Xing

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(+)-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.

Original languageEnglish (US)
Pages (from-to)7935-7940
Number of pages6
JournalJournal of medicinal chemistry
Issue number18
StatePublished - Jan 1 2017


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