Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/21825
Title: Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives
Authors: Wong, ILK
Wang, BC
Yuan, J
Duan, LX
Liu, Z
Liu, T
Li, XM
Hu, X
Zhang, XY
Jiang, T
Wan, SB
Chow, LMC 
Issue Date: 2015
Publisher: American Chemical Society
Source: Journal of medicinal chemistry, 2015, v. 58, no. 11, p. 4529-4549 How to cite?
Journal: Journal of Medicinal Chemistry 
Abstract: We are interested in developing novel natural product-derived P-gp inhibitors to reverse cancer drug resistance. Here, we have synthesized 55 novel derivatives of methylated epigallocatechin (EGC), gallocatechin (GC), and dihydromyricetin (DHM). Three EGC derivatives (23, 35, and 36) and three GC derivatives (50, 51, and 53) are significantly better than epigallocatechin gallate (EGCG) with a relative fold (RF) ranging from 31.4 to 53.6. The effective concentration (EC50) of 23 and 51 ranges from 102 to 195 nM. Compounds 23 and 51 are noncytotoxic to fibroblasts with IC50 > 100 μM. Compound 23 is specific for P-gp without modulating activity toward MRP1 or BCRP. Compounds 23 and 51 are non-P-gp substrates. Important pharmacophores for P-gp modulation were identified. In summary, methylated EGC and GC derivatives represent a new class of potent, specific, noncytotoxic, and nonsubstrate P-gp modulators.
URI: http://hdl.handle.net/10397/21825
ISSN: 0022-2623
DOI: 10.1021/acs.jmedchem.5b00085
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