European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry
5 years ago

Design and synthesis of conformationally constrained salinomycin derivatives

Design and synthesis of conformationally constrained salinomycin derivatives
Two conformationally restricted salinomycin derivatives by tethering the hydroxyl groups at C1 and C20 with different chain length were designed and synthesized. The cyclic derivatives showed better biological activities than C1/C20 modified derivatives, indicating the importance of the compact conformation for the ion binding capacity. In addition, the length of the connective chain plays critical role in the biological activities, thus cyclic the derivative 7 preserved some pharmacological activity but derivative 5 with two carbon atom shorter chain showed significantly reduced activity. The conformations of the two cyclic salinomycin derivatives were analyzed by ROESY spectrum in DMSO-d 6, indicating derivative 7 may adopt more appropriate conformations for the coordinate with alkali metal ion than derivative 5, which has a closer distance between H3 and H25.

Publisher URL: www.sciencedirect.com/science

DOI: S0223523417305172

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.