Synthesis of 1-O-acyl- and 1-oxo-kamebanin analogues and their cytotoxic activity

Bioorg Med Chem Lett. 2023 Feb 15:82:129149. doi: 10.1016/j.bmcl.2023.129149. Epub 2023 Jan 21.

Abstract

A series of 1-O-acyl- and 1-oxo-kamebanin analogues were prepared from kamebanin, isolated from Rabdosia excisa and their cytotoxicity was assayed on HL60 promyelocytic leukemia cells and HCT116 human colon cancer cells. The structure-activity relationship study showed that the presence of 1-O-acyl groups of a C3-C5 carbon chain increased the cytotoxic activity.

Keywords: Cytotoxicity; Ent-kaurene; Kamebanin; Semi-synthesis; Structure–activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • HCT116 Cells
  • HL-60 Cells
  • Humans
  • Isodon*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents