Design, synthesis and evaluation of a novel series of inhibitors reversing P‐glycoprotein‐mediated multidrug resistance | Zendy

Ghaleb Hesham | Zendy; Li Huilan | Zendy; Kairuki Mutta | Zendy; Qiu Qianqian | Zendy; Bi Xinzhou | Zendy; Liu Chunxia | Zendy; Liao Chen | Zendy; Li Jieming | Zendy; Hezam Kamal | Zendy; Huang Wenlong | Zendy; Qian Hai | Zendy

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Design, synthesis and evaluation of a novel series of inhibitors reversing P‐glycoprotein‐mediated multidrug resistance

Author(s) -

Ghaleb Hesham,

Li Huilan,

Kairuki Mutta,

Qiu Qianqian,

Bi Xinzhou,

Liu Chunxia,

Liao Chen,

Li Jieming,

Hezam Kamal,

Huang Wenlong,

Qian Hai

Publication year - 2018

Publication title -

chemical biology and drug design

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.59

H-Index - 77

eISSN - 1747-0285

pISSN - 1747-0277

DOI - 10.1111/cbdd.13338

Subject(s) - p glycoprotein , multiple drug resistance , efflux , verapamil , pharmacology , doxorubicin , chemistry , cytotoxic t cell , drug resistance , chemotherapy , medicine , biochemistry , biology , in vitro , organic chemistry , microbiology and biotechnology , calcium , antibiotics

Multidrug resistance ( MDR ) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo‐reversal agents is needed to overcome MDR . Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil ( VRP ) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells. Compound 19 also played an important role in the P‐gp efflux function of intracellular Rh123 and doxorubicin ( DOX ) accumulation in K562/A02 cells. Moreover, compound 19 exhibited a long lifetime of approximately 24 hr. These results indicated that compound 19 is a potential lead compound for the design of new drugs to overcome cancer MDR .

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