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

Pilot in Vivo Structure-Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O 6-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

J Med Chem. 2017 Sep 28;60(18):7935-7940.

PMID: 28806079

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP19902911-A	(+)-Dihydromethysticin		19902-91-1	Price

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