Design and synthesis of novel magnolol derivatives as potential antimicrobial and antiproliferative compounds

A series of novel magnolol derivatives were synthesised and evaluated for in vitro antimicrobial and antiproliferative activities. We found that most of the compounds were effective inhibitors of Staphylococcus aureus, MRSA and VRE with MIC in the range of 1–64 μg/mL and MBC in the range of 1–128 μg/mL. Few derivatives also exhibited promising antifungal activity. Some magnolol analogues exhibited promising antiproliferative activity than parent magnolol when tested against three human cancer cell lines.

Graphical abstractA series of magnolol derivatives were synthesised and evaluated for antimicrobial and antiproliferative activities. Many analogues exhibited promising antibacterial activity against multi-drug resistant bacteria and few derivatives showed significant antiproliferative and antifungal activity.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Present manuscript highlights the synthesis, in vitro antimicrobial and antiproliferative studies of magnolol derivatives. ► Most of the compounds exhibited significant antibacterial activity against Staphylococcus aureus ATCC, MRSA and VRE. ► Few compounds exhibited promising antifungal activity. ► Some halogen substituted derivatives showed improved antiproliferative activity as compared to magnolol. ► DNA laddering and flow cytometric studies established the apoptotic mechanism of cell killing.