Aniline-containing derivatives of parthenolide: Synthesis and anti-chronic lymphocytic leukaemia activity.

ABSTRACT: Parthenolide exhibits anti-leukaemia activity, whilst its synthetic modification to impart improve drug-like properties, including 1,4-conjugate addition of primary and secondary amines, have previously been used, 1,4-addition of aniline derivatives to parthenolide has not been fully explored. A protocol for such additions to parthenolide is outlined herein. Reaction conditions were determined using tulipane as a model Michael acceptor. Subsequently, aniline-containing parthenolide derivatives were prepared under the optimised conditions and single crystal X-ray diffraction structures were resolved for three of the compounds synthesised. The synthesised derivatives, along with compounds resulting from a side reaction, were tested for their in vitro anti-leukaemia activity using the chronic

SUBMITTER: Quy AS 

PROVIDER: S-EPMC7695678 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature