Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2

  • Bioorg Med Chem Lett. 2000 Jan 3;10(1):39-43. doi: 10.1016/s0960-894x(99)00577-6.
C K Han  1 ,  S K Ahn ,  N S Choi ,  R K Hong ,  S K Moon ,  H S Chun ,  S J Lee ,  J W Kim ,  C I Hong ,  D Kim ,  J H Yoon ,  K T No
Affiliations
  • 1. Chong Kun Dang Research Institute, Chungcheongnamdo, South Korea.
PMID: 10636239 DOI: 10.1016/s0960-894x(99)00577-6
Abstract

New fumagillin analogues were designed through structure-based molecular modeling with a human methionine aminopeptidase-2. Among the fumagillin analogues, cinnamic acid ester derivative CKD-731 showed 1000-fold more potent proliferation inhibitory activity on endothelial cell than TNP-470.

Products