Search Results - "Zhang, Daoguang"
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Discovery of novel pyrazole derivatives as potential anticancer agents in MCL
Published in Bioorganic & medicinal chemistry letters (01-05-2019)“…[Display omitted] Mantle cell lymphoma (MCL) is characterized by the translocation t(11;14) (q13;q32), resulting in the overexpression of cyclin-D1. The…”
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Recent Developments in Androgen Receptor Antagonists
Published in Archiv der Pharmazie (Weinheim) (01-11-2015)“…The androgen receptor (AR), a ligand‐dependent transcription factor that regulates the expression of a series of downstream target genes after the binding of…”
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Discovery of pyrazolopyrimidine derivatives as potent BTK inhibitors with effective anticancer activity in MCL
Published in Bioorganic chemistry (01-08-2019)“…[Display omitted] •Pyrazolopyrimidine derivatives as potent BTK inhibitors.•12a obtained antiproliferative effects in primary patient tumor cells.•12a showed…”
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Targeting Bruton's tyrosine kinase for the treatment of B cell associated malignancies and autoimmune diseases: Preclinical and clinical developments of small molecule inhibitors
Published in Archiv der Pharmazie (Weinheim) (01-07-2018)“…B cell receptor (BCR) signaling plays a key role in B cell development and function. Aberrant BCR signaling has been confirmed as a central driver for the…”
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Structural optimization elaborates novel potent Akt inhibitors with promising anticancer activity
Published in European journal of medicinal chemistry (29-09-2017)“…Targeting of Akt has been validated as a well rationalized approach to cancer treatment, and represents a promising therapeutic strategy for aggressive…”
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Synthesis and biological evaluation of 3-(4-fluorophenyl)-1H-pyrazole derivatives as androgen receptor antagonists
Published in Anti-cancer drugs (01-04-2016)“…A novel series of 3-(4-fluorophenyl)-1H-pyrazole derivatives were synthesized and evaluated for their antiproliferative activity against two prostate cancer…”
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Discovery of novel 5‐methyl‐1 H ‐pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation
Published in Chemical biology & drug design (01-06-2018)“…Androgen receptor ( AR ) signaling functions as a core driving force for the progression of prostate cancer ( PC a), and AR has been proved to be an effective…”
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Discovery of novel 5‐methyl‐1H‐pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation
Published in Chemical biology & drug design (01-06-2018)“…Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective…”
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Discovery of novel 5-methyl-1H-pyrazole derivatives as potential anti-prostate cancer agents: design, synthesis, molecular modeling and biological evaluation
Published in Chemical biology & drug design (2018)“…Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective…”
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Design, synthesis and biological evaluation of AKT inhibitors bearing a piperidin-4-yl appendant
Published in MedChemComm (01-08-2018)“…A series of AKT inhibitors possessing a piperidin-4-yl side chain was designed and synthesized. Some of them showed high AKT1 inhibitory activity and potent…”
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Design and discovery of 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide inhibitors of HIV-1 integrase
Published in Bioorganic & medicinal chemistry (01-10-2014)“…Raltegravir (RAL) is a first clinically approved integrase (IN) inhibitor for the treatment of HIV but rapid mutation of the virus has led to chemo-resistant…”
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Design, synthesis, and biological evaluation of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives as androgen receptor antagonists
Published in Medicinal chemistry research (15-03-2019)“…Androgen receptor (AR) signaling is often activated in prostate cancer (PCa) cells, and blockage of this signaling by AR antagonists is an important strategy…”
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