Synthesis and biological evaluation of novel symmetry bis-enediynes

A series of acyclic symmetry bis-enediynes have been synthesized successfully and their bioactivities were evaluated. Among them, 1,6-bis(4-((2-(pyridin-2-ylethynyl)phenyl)ethynyl)phenoxy)hexane 8g showed good inhibition activity against the CCRF-CEM (GI50 = 0.04 μM) and HL-60 (GI50 = 0.09 μM) cell lines of human leukemia. The cell cycle analysis shows that compound 8g arrests cell cycle via inhibiting Cyclin A and Cyclin B expressions in low concentration and induces a significant apoptosis progress in high concentration.

Graphical abstractBis-enediyne 1g showed most potent growth inhibition activity against all tumor cell lines in low concentration, blocked cell cycle via controlling Cyclin A and Cyclin B expressions and induced apoptosis phenomenon in high concentration.Figure optionsDownload full-size imageDownload as PowerPoint slide