Design and synthesis of a novel curcumin-combretastatin A4 molecular skeleton: two pharmacophores.

ABSTRACT: The logical design and synthesis of a novel compound combretastatin A-4-integrated curcumin is presented. Claisen condensation of phenylacetone with ethyl acetates formed 1,5-diphenylpentane-2,4-dione. Condensation of the dione with benzaldehyde via a modified Pabon procedure formed combretastatin A-4-integrated curcumin. The single-crystal X-ray structure of one of the CA-4 integrated CURs was established as a representative example. Curcumin (CUR) and combretastatin A-4 (CA-4) are well-known bioactive natural products; however, their poor pharmacokinetic profiles and cis-trans isomerization under in vivo conditions, respectively, have limited their biological applications. Herein, coupling of an aryl group at the olefinic C2 and/or C6 position of CUR integrate

SUBMITTER: Ponraj P 

PROVIDER: S-EPMC11578218 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature