Antitumor agents. Part 218: Cappamensin A, a new In vitro anticancer principle, from Capparis sikkimensis

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2223-5. doi: 10.1016/s0960-894x(03)00379-2.

Abstract

A new inhibitor of in vitro tumor cell replication, cappamensin A (1) (2H-1,4-benzoxazin-3(4H)-one, 6-methoxy-2-methyl-4-carbaldehyde), was isolated from the roots of Capparis sikkimensis subsp. formosana using bioactivity-guided fractionation. The structure of 1 was established by spectroscopic methods, including 2D NMR analyses. Compound 1 displayed significant in vitro anticancer activity against ovarian (1A9), lung (A549), ileocecal (HCT-8), breast (MCF-7), nasopharyngeal (KB), and vincristine resistant (KB-VIN) human tumor cell lines with ED(50) values </=4 microgram/mL (mean GI(50) value of 15.1 microM).

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aldehydes / chemistry*
  • Aldehydes / pharmacology*
  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Benzoxazines
  • Capparis / chemistry*
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Magnetic Resonance Spectroscopy
  • Molecular Conformation
  • Oxazines / chemistry*
  • Oxazines / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • 2H-1,4-benzoxazin-3(4H)-one, 6-methoxy-2-methyl-4-carbaldehyde
  • Aldehydes
  • Antineoplastic Agents, Phytogenic
  • Benzoxazines
  • Oxazines