Synthesis of curcumin mimics with multidrug resistance reversal activities.
In order to discover novel multidrug resistance (MDR) reversal agents for efficient cancer chemotherapy, the unsymmetrical curcumin mimics with various amide moieties (6-19) were synthesized and evaluated their MDR reversal activities in MDR cell line KBV20C. Among the tested compounds, 13, 16, and 17 showed potent MDR reversal activities by inhibiting drug efflux function of P-glycoprotein in KB20C cells, and almost recovered the cytotoxicity of vincristine and paclitaxel against KBV20C cell to the degree of potency against drug sensitive KB cells.
Um
Yumi
Y
College of Medicine, Kwandong University, Gangneung 210-701, Republic of Korea.
Cho
Sungsik
S
Woo
Ho Bum
HB
Kim
Yong Kee
YK
Kim
Hanna
H
Ham
Jungyeob
J
Kim
Su-Nam
SN
Ahn
Chan Mug
CM
Lee
Seokjoon
S
D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003432:Cross-Linking Reagents / Q000737:chemistry; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D013237:Stereoisomerism
D003432:Cross-Linking Reagents; D003474:Curcumin