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Synthesis and Evaluation of Dibenzothiophene Analogues as Pin1 Inhibitors for Cervical Cancer Therapy
Wu, KJ1; Liu, X2; Wong, SY3; Zhou, YY2; Ma, DL3; Leung, CH1
2019
Source PublicationACS OMEGA
ISSN2470-1343
Volume4Issue:5Pages:9228-9234
AbstractThe peptidyl-prolyl isomerase Pin1 is correlated with the progression of cervical cancer via regulating numerous oncogenic and tumor suppressor pathways. p65 is a crucial regulator of tumorigenesis that is regulated by Pin1, and p65 signaling suppression can enhance the antitumor efficacy of doxorubicin (DOX). Here, we utilized a structural mimicry approach to synthesize a series of dibenzothiophene analogues and evaluated their ability to inhibit Pin1 activity. Compound 1a was identified as a potent Pin1 inhibitor that inhibited p65 signaling in vitro and in cervical cancer cells. Moreover, compound 1a enhanced the cytotoxicity of DOX in cervical cancer cells via reducing p65 nuclear accumulation and enhancing DOX uptake. These compounds are promising scaffolds for developing more potent Pin1 inhibitors against cervical cancer, either alone or in combination with anticancer drugs such as DOX.
DOI10.1021/acsomega.9b00281
Indexed BySCI
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000470094000148
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Cited Times [WOS]:1   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorMa, DL
Affiliation1.University of Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau 999078, Peoples R China
2.Suzhou Univ Sci & Technol, Sch Chem Biol & Mat Engn, 1 Kerui Rd, Suzhou 215009, Jiangsu, Peoples R China
3.Hong Kong Baptist Univ, Dept Chem, Kowloon Tong, Hong Kong 999077, Peoples R China
First Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Wu, KJ,Liu, X,Wong, SY,et al. Synthesis and Evaluation of Dibenzothiophene Analogues as Pin1 Inhibitors for Cervical Cancer Therapy[J]. ACS OMEGA,2019,4(5):9228-9234.
APA Wu, KJ,Liu, X,Wong, SY,Zhou, YY,Ma, DL,&Leung, CH.(2019).Synthesis and Evaluation of Dibenzothiophene Analogues as Pin1 Inhibitors for Cervical Cancer Therapy.ACS OMEGA,4(5),9228-9234.
MLA Wu, KJ,et al."Synthesis and Evaluation of Dibenzothiophene Analogues as Pin1 Inhibitors for Cervical Cancer Therapy".ACS OMEGA 4.5(2019):9228-9234.
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