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 (GI(50)=0.04 microM) and HL-60 (GI(50)=0.09 microM) 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.
Tseng
Kuo-Feng
KF
Faculty of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
Lin
Chi-Fong
CF
Lo
Yu-Hsiang
YH
Hu
Yi-Ling
YL
Chen
Li-Yi
LY
Yang
Sheng-Huei
SH
Lin
Shinne-Ren
SR
Chang
Long-Sen
LS
Wu
Ming-Jung
MJ
D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D019925:Cyclin A / Q000037:antagonists & inhibitors; D019926:Cyclin B / Q000037:antagonists & inhibitors; D004305:Dose-Response Relationship, Drug; D053281:Enediynes / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007938:Leukemia / Q000188:drug therapy* / Q000473:pathology
D019925:Cyclin A; D019926:Cyclin B; D053281:Enediynes