Literature DB >> 23375227

Critical role of a methyl group on the γ-lactone ring of annonaceous acetogenins in the potent inhibition of mitochondrial complex I.

Naoto Kojima1, Masato Abe, Yuki Suga, Kazufumi Ohtsuki, Tetsuaki Tanaka, Hiroki Iwasaki, Masayuki Yamashita, Hideto Miyoshi.   

Abstract

C34-epi and C34-epi-C35-trifluoro analogues of solamin, a mono-THF annonaceous acetogenin, were synthesized. Their inhibitory activity, along with previously synthesized analogues (C35-fluoro, C35-difluoro, and C35-trifluorosolamins), against bovine mitochondrial NADH-ubiquinone oxidoreductase (complex I) was determined. The present study revealed that the methyl group on the γ-lactone moiety is critical to the potent inhibition of complex I by natural acetogenins.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2013        PMID: 23375227     DOI: 10.1016/j.bmcl.2013.01.018

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Structure-antitumor activity relationship of hybrid acetogenins focusing on connecting groups between heterocycles and the linker moiety.

Authors:  Kaito Ohta; Tetsuya Fushimi; Mutsumi Okamura; Akinobu Akatsuka; Shingo Dan; Hiroki Iwasaki; Masayuki Yamashita; Naoto Kojima
Journal:  RSC Adv       Date:  2022-05-25       Impact factor: 4.036

2.  Photo-affinity labelling and biochemical analyses identify the target of trypanocidal simplified natural product analogues.

Authors:  Lindsay B Tulloch; Stefanie K Menzies; Andrew L Fraser; Eoin R Gould; Elizabeth F King; Marija K Zacharova; Gordon J Florence; Terry K Smith
Journal:  PLoS Negl Trop Dis       Date:  2017-09-05
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.