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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.


ABSTRACT: (+)-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.

SUBMITTER: Puppala M 

PROVIDER: S-EPMC5729742 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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Pilot in Vivo Structure-Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O<sup>6</sup>-Methylguanine and Lung Tumor in A/J Mice.

Puppala Manohar M   Narayanapillai Sreekanth C SC   Leitzman Pablo P   Sun Haifeng H   Upadhyaya Pramod P   O'Sullivan M Gerard MG   Hecht Stephen S SS   Xing Chengguo C  

Journal of medicinal chemistry 20170913 18


(+)-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 O<sup>6</sup>-methylguanine and long-term adenoma formation in the lung tissues in A/J mice. Both results revealed cohesive SARs, demonstrating that the methylenediox  ...[more]

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