Skip NavigationSkip to Content
Return Return to Search Results

Chemical synthesis and biological properties of pyridine epothilones

  1. Author:
    Nicolaou, K. C.
    Scarpelli, R.
    Bollbuck, B.
    Werschkun, B.
    Pereira, M. M. A.
    Wartmann, M.
    Altmann, K. H.
    Zaharevitz, D.
    Gussio, R.
    Giannakakou, P.

  2. Author Address

    Scripps Res Inst, Dept Chem, 10550 N Torrey Pines Rd, La Jolla, CA 92037 USA. Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA. Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA. Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA. Novartis Pharma AG, TA Oncol Res, CH-4002 Basel, Switzerland. NCI, Target Struct Based Drug Discovery Grp, Informat Technol Branch, Dev Therapeut Program, NIH, Frederick, MD 21702 USA. NCI, Med Branch, NIH, Bethesda, MD 20892 USA.
    1. Year: 2000
  2. Journal: Chemistry & Biology
    1. 7
    2. 8
    3. Pages: 593-599
  4. Type of Article: Article
  1. Abstract:

    Background: Numerous analogs of the antitumor agents epothilones A and B have been synthesized in search of better pharmacological profiles. Insights into the structure-activity relationships within the epothilone family are still needed and more potent and selective analogs of these compounds are in demand, both as biological tools and as chemotherapeutic agents, especially against drug-resistant tumors, Results: A series of pyridine epothilone B analogs were designed, synthesized and screened. The synthesized compounds exhibited varying degrees of tubulin polymerization and cytotoxicity properties against a number of human cancer cell lines depending on the location of the nitrogen atom and the methyl substituent within the pyridine nucleus. Conclusions: The biological screening results in this study established the importance of the nitrogen atom at the ortho position as well as the beneficial effect of a methyl substituent at the 4- or 5-position of the pyridine ring. Two pyridine epothilone B analogs (i.e. compounds 3 and 4) possessing higher potencies against drug-resistant tumor cells than epothilone B, the most powerful of the naturally occurring epothilones, were identified.

    See More

  1. Keywords:

External Sources

  1. No sources found.

Library Notes

  1. No notes added.
NCI at Frederick

You are leaving a government website.

This external link provides additional information that is consistent with the intended purpose of this site. The government cannot attest to the accuracy of a non-federal site.

Linking to a non-federal site does not constitute an endorsement by this institution or any of its employees of the sponsors or the information and products presented on the site. You will be subject to the destination site's privacy policy when you follow the link.

ContinueCancel