Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors

Chao Yang; Iris L.K. Wong; Wen Bin Jin; Tao Jiang; Ming Cheung Chow; Sheng Biao Wan

doi:10.3390/md12105209

Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors

Chao Yang, Iris L.K. Wong, Wen Bin Jin, Tao Jiang, Ming Cheung Chow, Sheng Biao Wan

Research output: Journal article publication › Journal article › Academic research › peer-review

10 Citations (Scopus)

Abstract

In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.

Original language	English
Pages (from-to)	5209-5221
Number of pages	13
Journal	Marine Drugs
Volume	12
Issue number	10
DOIs	https://doi.org/10.3390/md12105209
Publication status	Published - 17 Oct 2014

Keywords

Multidrug resistance (MDR)
Ningalin B analogues
P-glycoprotein
P-gp modulators
Pyrrole

ASJC Scopus subject areas

Drug Discovery

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

More information

10.3390/md12105209

http://hdl.handle.net/10397/36131

Cite this

@article{d10b36052e894209911b25850fefea16,

title = "Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors",

abstract = "In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.",

keywords = "Multidrug resistance (MDR), Ningalin B analogues, P-glycoprotein, P-gp modulators, Pyrrole",

author = "Chao Yang and Wong, {Iris L.K.} and Jin, {Wen Bin} and Tao Jiang and Chow, {Ming Cheung} and Wan, {Sheng Biao}",

year = "2014",

month = oct,

day = "17",

doi = "10.3390/md12105209",

language = "English",

volume = "12",

pages = "5209--5221",

journal = "Marine Drugs",

issn = "1660-3397",

publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",

number = "10",

}

TY - JOUR

T1 - Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors

AU - Yang, Chao

AU - Wong, Iris L.K.

AU - Jin, Wen Bin

AU - Jiang, Tao

AU - Chow, Ming Cheung

AU - Wan, Sheng Biao

PY - 2014/10/17

Y1 - 2014/10/17

N2 - In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.

AB - In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.

KW - Multidrug resistance (MDR)

KW - Ningalin B analogues

KW - P-glycoprotein

KW - P-gp modulators

KW - Pyrrole

UR - http://www.scopus.com/inward/record.url?scp=84908199216&partnerID=8YFLogxK

U2 - 10.3390/md12105209

DO - 10.3390/md12105209

M3 - Journal article

C2 - 25329704

SN - 1660-3397

VL - 12

SP - 5209

EP - 5221

JO - Marine Drugs

JF - Marine Drugs

IS - 10

ER -

Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

More information

Other files and links

Fingerprint

Cite this