Synthesis of novel diaryl ethers and their evaluation as antimitotic agents.
A series of novel diaryl ethers possessing various functional groups were synthesized and evaluated for antiproliferative activity in human myeloid leukemia HL-60 cells. Among the compounds examined, compounds 10, 17, 20, 24, and 33 showed moderate to potent antiproliferative activity. These derivatives were further examined in terms of their abilities to inhibit tubulin polymerization; however, all of the tested compounds were relatively ineffective. The reference compound E7010 with an IC(50) of 0.34 microM exhibited potent antiproliferative activity and significantly inhibited tubulin polymerization in a dose-dependent manner.
In
Jin-Kyung
JK
College of Pharmacy, Chungbuk National University, Cheongju 361-763, Republic of Korea. orgjkjung@chungbuk.ac.kr
Lee
Mi-Sung
MS
Yang
Jung-Eun
JE
Kwak
Jae-Hwan
JH
Lee
Heesoon
H
Boovanahalli
Shanthaveerappa K
SK
Lee
Kyeong
K
Kim
Soo Jin
SJ
Moon
Seung Kee
SK
Lee
Sungsook
S
Choi
Nam Song
NS
Ahn
Soon Kil
SK
Jung
Jae-Kyung
JK
D050256:Antimitotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004987:Ethers / Q000138:chemical synthesis* / Q000494:pharmacology*; D018922:HL-60 Cells; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008938:Mitosis / Q000187:drug effects; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000096:biosynthesis
D050256:Antimitotic Agents; D004987:Ethers; D007202:Indicators and Reagents; D014404:Tubulin