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Synthesis of curcumin mimics with multidrug resistance reversal activities

Authors
Um, Yumi; Cho, Sungsik; Woo, Ho Bum; Kim, Yong Kee; Kim, Hanna; Ham, Jungyeob; Kim, Su-Nam; Ahn, Chan Mug; Lee, Seokjoon
Issue Date
2008-04-01
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY, v.16, no.7, pp.3608 - 3615
Abstract
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. (C) 2008 Elsevier Ltd. All rights reserved.
Keywords
P-GLYCOPROTEIN; BIOLOGICAL EVALUATION; CANCER-CELLS; DERIVATIVES; ANTICANCER; MODULATION; INHIBITION; THERAPY; ANALOGS; AGENTS; P-GLYCOPROTEIN; BIOLOGICAL EVALUATION; CANCER-CELLS; DERIVATIVES; ANTICANCER; MODULATION; INHIBITION; THERAPY; ANALOGS; AGENTS; curcumin; curcumin mimics; multidrug resistance; multidrug resistance reversal activities; anticancer
ISSN
0968-0896
URI
https://pubs.kist.re.kr/handle/201004/133564
DOI
10.1016/j.bmc.2008.02.012
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KIST Article > 2008
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