Synthesis and cytotoxicity of 2,5-dihydroxychalcones and related compounds.
A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cytotoxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC) evaluated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2'-chloro-2, 5-dihydroxychalcone (9) was most potent, with an IC50 value as low as 0.31 microg/mL. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.
Nam
Nguyen-Hai
NH
College of Pharmacy, Chungnam National University, Taejon 305-764, Korea.
Hong
Dong-Ho
DH
You
Young-Jae
YJ
Kim
Yong
Y
Bang
Seong-Cheol
SC
Kim
Hwan-Mook
HM
Ahn
Byung-Zun
BZ
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002599:Chalcone / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047188:Chalcones; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects; D006801:Humans; D051379:Mice; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014471:Umbilical Veins / Q000166:cytology
C107497:2',5'-dihydroxychalcone; D000970:Antineoplastic Agents; D047188:Chalcones; D002599:Chalcone