2. Academic Validation
  3. Identification of novel and improved antimitotic agents derived from noscapine

Identification of novel and improved antimitotic agents derived from noscapine

  • J Med Chem. 2005 Nov 17;48(23):7096-8. doi: 10.1021/jm050674q.
James T Anderson 1,  Anthony E Ting,  Sherry Boozer,  Kurt R Brunden,  Chris Crumrine,  Joel Danzig,  Tom Dent,  Laurel Faga,  John J Harrington,  William F Hodnick,  Steven M Murphy,  Gary Pawlowski,  Robert Perry,  Amy Raber,  Stephen E Rundlett,  Alain Stricker-Krongrad,  Jianmin Wang,  Youssef L Bennani
Affiliations

Affiliation

  • 1 Athersys, Inc., 3201 Carnegie Avenue, Cleveland, Ohio 44115-2634, USA. janderson@athersys.com
PMID: 16279766 DOI: 10.1021/jm050674q
Abstract

Analogues of the natural product noscapine were synthesized and their potential as antitumor agents evaluated. The discovery of a novel regioselective O-demethylation facilitated the synthesis of the potent aniline 6, which arrests mammalian cells in the G2/M phase of the cell cycle at 0.1 microM and also affects tubulin polymerization. Aniline 6 is orally bioavailable and is 250-fold more potent than noscapine in reducing cell proliferation in rapidly dividing cells.

Figures