Bis-styrylpyridine and bis-styrylbenzene derivatives as inhibitors for Abeta fibril formation.
New bis-styrylpyridine and bis-styrylbenzene derivatives were designed and synthesized. These 34 compounds were evaluated by Abeta fibril formation inhibitory assay using thioflavin T as a dye (named ThT assay). Most of them showed excellent inhibitory activities for Abeta fibril formation at IC50 of 0.1-2.7 microM which is comparable to curcumin (IC50 of 0.8 microM). Among them, nine compounds were screened for their cytotoxicities on HT-22 cell by MTT assay at 1, 10, and 50 microM. In particular, I-7 and II-2 exhibited the best combination of inhibitory activity and compound cytotoxicity.
Byeon
Seong Rim
SR
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, P.O. Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Lee
Ji Hoon
JH
Sohn
Ji-Hoon
JH
Kim
Dong Chan
DC
Shin
Kye Jung
KJ
Yoo
Kyung Ho
KH
Mook-Jung
Inhee
I
Lee
Won Koo
WK
Kim
Dong Jin
DJ
D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors*; D000818:Animals; D001555:Benzene Derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D052160:Benzothiazoles; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D020128:Inhibitory Concentration 50; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis / Q000494:pharmacology; D013844:Thiazoles
D016229:Amyloid beta-Peptides; D001555:Benzene Derivatives; D052160:Benzothiazoles; D011725:Pyridines; D013343:Styrenes; D013844:Thiazoles; C009462:thioflavin T