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10.1016/j.ejmech.2021.113267 http://scihub22266oqcxt.onion/10.1016/j.ejmech.2021.113267 33639344!7873610!33639344     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=33639344&cmd=llinks): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 215 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 229.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Eur+J+Med+Chem 2021 ; 215 (ä): 113267 Nephropedia Template TP {{tp|p=33639344|t=2021. A new class of alpha-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities |pdf=|usr=}}{{33639344}} gab.com Text A new class of alpha-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities JO: Eur J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=33639344 #FOAvip Inhibitors of the proteasome have been extensively studied for their applications in the treatment of human diseases such as hematologic malignancies, autoimmune disorders, and viral infections. Many of the proteasome inhibitors reported in the literature target the non-primed site of proteasome's substrate binding pocket. In this study, we designed, synthesized and characterized a series of novel alpha-keto phenylamide derivatives aimed at both the primed and non-primed sites of the proteasome. In these derivatives, different substituted phenyl groups at the head group targeting the primed site were incorporated in order to investigate their structure-activity relationship and optimize the potency of alpha-keto phenylamides. In addition, the biological effects of modifications at the cap moiety, P1, P2 and P3 side chain positions were explored. Many derivatives displayed highly potent biological activities in proteasome inhibition and anticancer activity against a panel of six cancer cell lines, which were further rationalized by molecular modeling analyses. Furthermore, a representative alpha-ketoamide derivative was tested and found to be active in inhibiting the cellular infection of SARS-CoV-2 which causes the COVID-19 pandemic. These results demonstrate that this new class of alpha-ketoamide derivatives are potent anticancer agents and provide experimental evidence of the anti-SARS-CoV-2 effect by one of them, thus suggesting a possible new lead to develop antiviral therapeutics for COVID-19. Twit Text FOAVip A new class of alpha-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities ????Eur J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=33639344 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33639344 #FOAvip English Wikipedia <ref>{{Cite pmid|33639344}}</ref> A new class of alpha-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities #MMPMID33639344 Wang J; Liang B; Chen Y; Fuk-Woo Chan J; Yuan S; Ye H; Nie L; Zhou J; Wu Y; Wu M; Huang LS; An J; Warshel A; Yuen KY; Ciechanover A; Huang Z; Xu Y Eur J Med Chem 2021[Apr]; 215 (ä): 113267 PMID33639344show ga Inhibitors of the proteasome have been extensively studied for their applications in the treatment of human diseases such as hematologic malignancies, autoimmune disorders, and viral infections. Many of the proteasome inhibitors reported in the literature target the non-primed site of proteasome's substrate binding pocket. In this study, we designed, synthesized and characterized a series of novel alpha-keto phenylamide derivatives aimed at both the primed and non-primed sites of the proteasome. In these derivatives, different substituted phenyl groups at the head group targeting the primed site were incorporated in order to investigate their structure-activity relationship and optimize the potency of alpha-keto phenylamides. In addition, the biological effects of modifications at the cap moiety, P1, P2 and P3 side chain positions were explored. Many derivatives displayed highly potent biological activities in proteasome inhibition and anticancer activity against a panel of six cancer cell lines, which were further rationalized by molecular modeling analyses. Furthermore, a representative alpha-ketoamide derivative was tested and found to be active in inhibiting the cellular infection of SARS-CoV-2 which causes the COVID-19 pandemic. These results demonstrate that this new class of alpha-ketoamide derivatives are potent anticancer agents and provide experimental evidence of the anti-SARS-CoV-2 effect by one of them, thus suggesting a possible new lead to develop antiviral therapeutics for COVID-19. |Amides/chemical synthesis/metabolism/*pharmacology[MESH] |Antineoplastic Agents/chemical synthesis/metabolism/*pharmacology[MESH] |Antiviral Agents/chemical synthesis/metabolism/*pharmacology[MESH] |Binding Sites[MESH] |Calpain/chemistry/metabolism[MESH] |Cell Line, Tumor[MESH] |Coronavirus 3C Proteases/chemistry/metabolism[MESH] |Drug Screening Assays, Antitumor[MESH] |Humans[MESH] |Ketones/chemical synthesis/metabolism/*pharmacology[MESH] |Microbial Sensitivity Tests[MESH] |Molecular Docking Simulation[MESH] |Molecular Dynamics Simulation[MESH] |Molecular Structure[MESH] |Proteasome Endopeptidase Complex/chemistry/metabolism[MESH] |Proteasome Inhibitors/chemical synthesis/metabolism/*pharmacology[MESH] |Protein Binding[MESH] |SARS-CoV-2/*drug effects[MESH]A new class of alpha-ketoamide derivatives with potent anticancer and (epmc).pdf DeepDyve Pubget Overpricing