國家衛生研究院 NHRI:Item 3990099045/11771
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    題名: Synthesis and evaluation of novel 7H-pyrrolo-[2,3-d]pyrimidine derivatives as potential anticancer agents
    作者: Liu, YM;Chen, CH;Yeh, TK;Liou, JP
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: AIM: Bladder cancer is a highly recurrent urologic malignancy with limited treatment approaches. Previously, we reported compound 11 is a FGFR3 inhibitor with significant antibladder cancer activity. MATERIALS & METHODS: In this study, a series of 7H-pyrrolo-[2,3-d]pyrimidine derivatives were synthesized through ring formation and modification of compound 11 for anticancer activity evaluation. RESULTS: Compound 13i is the most effective agent against human RT-112 bladder cancer cells. Notably, 13i strongly inhibits CK1delta without affecting FGFR3 activity. We generated 13i HCl to increase solubility and showed profound cell cycle accumulation at the sub-G1 phase and apoptosis in CK1delta-overexpressed bladder and ovarian cancer cells. CONCLUSION: These results indicate that compound 13i could be a lead compound for further development of novel anticancer agents.
    日期: 2019-05
    關聯: Future Medicinal Chemistry. 2019 May;11(9):959-974.
    Link to: http://dx.doi.org/10.4155/fmc-2018-0564
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1756-8919&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000474891700005
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85067596772
    顯示於類別:[葉燈光] 期刊論文

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