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10.1080/14756366.2017.1347166 http://scihub22266oqcxt.onion/10.1080/14756366.2017.1347166 C6010115!6010115 !28726519     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=28726519 &cmd=llinks): Failed to open stream: HTTP request failed! 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Cancer stem cells CD133 inhibition and cytotoxicity of certain 3-phenylthiazolo 3,2-a benzimidazoles: design, direct synthesis, crystal study and in vitro biological evaluation |pdf=|usr=}}{{28726519 }} gab.com Text Cancer stem cells CD133 inhibition and cytotoxicity of certain 3-phenylthiazolo 3,2-a benzimidazoles: design, direct synthesis, crystal study and in vitro biological evaluation JO: J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=28726519 #FOAvip Cancer stem cells (CSCs) have been objects of intensive study since their identification in 1994. Adopting a structural rigidification approach, a novel series of 3-phenylthiazolo[3,2-a]benzimidazoles 4a-d was designed and synthesised, in an attempt to develop potent anticancer agent that can target the bulk of tumour cells and CSCs. The anti-proliferative activity of the synthesised compounds was evaluated against two cell lines, namely; colon cancer HT-29 and triple negative breast cancer MDA-MB-468 cell lines. Also, their inhibitory activity against the cell surface expression of CD133 was examined. In particular, compound 4b emerged as a promising hit molecule as it manifested good antineoplastic potency against both tested cell lines (IC(50)?=?9 and 12??M, respectively), beside its ability to inhibit the cell surface expression of CD133 by 50% suggesting a promising potential of effectively controlling the tumour by eradicating the tumour bulk and inhibiting the proliferation of the CSCs. Moreover, compounds 4a and 4c showed moderate activity against HT-29 (IC(50)?=?21 and 29??M, respectively) and MDA-MB-468 (IC(50)?=?23 and 24??M, respectively) cell lines, while they inhibited the CD133 expression by 14% and 48%, respectively. Finally, a single crystal X-ray diffraction was recorded for compound 4d. Twit Text FOAVip Cancer stem cells CD133 inhibition and cytotoxicity of certain 3-phenylthiazolo 3,2-a benzimidazoles: design, direct synthesis, crystal study and in vitro biological evaluation ????J Enzyme Inhib Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=28726519 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=28726519 #FOAvip English Wikipedia <ref>{{Cite pmid|28726519 }}</ref> Cancer stem cells CD133 inhibition and cytotoxicity of certain 3-phenylthiazolo 3,2-a benzimidazoles: design, direct synthesis, crystal study and in vitro biological evaluation #MMPMID28726519 Al-Ansary GH ; Eldehna WM ; Ghabbour HA ; Al-Rashood STA ; Al-Rashood KA ; Eladwy RA ; Al-Dhfyan A ; Kabil MM ; Abdel-Aziz HA J Enzyme Inhib Med Chem 2017[Dec]; 32 (1 ): 986-991 PMID28726519 show ga Cancer stem cells (CSCs) have been objects of intensive study since their identification in 1994. Adopting a structural rigidification approach, a novel series of 3-phenylthiazolo[3,2-a]benzimidazoles 4a-d was designed and synthesised, in an attempt to develop potent anticancer agent that can target the bulk of tumour cells and CSCs. The anti-proliferative activity of the synthesised compounds was evaluated against two cell lines, namely; colon cancer HT-29 and triple negative breast cancer MDA-MB-468 cell lines. Also, their inhibitory activity against the cell surface expression of CD133 was examined. In particular, compound 4b emerged as a promising hit molecule as it manifested good antineoplastic potency against both tested cell lines (IC(50)?=?9 and 12??M, respectively), beside its ability to inhibit the cell surface expression of CD133 by 50% suggesting a promising potential of effectively controlling the tumour by eradicating the tumour bulk and inhibiting the proliferation of the CSCs. Moreover, compounds 4a and 4c showed moderate activity against HT-29 (IC(50)?=?21 and 29??M, respectively) and MDA-MB-468 (IC(50)?=?23 and 24??M, respectively) cell lines, while they inhibited the CD133 expression by 14% and 48%, respectively. Finally, a single crystal X-ray diffraction was recorded for compound 4d. |*Drug Design [MESH] |AC133 Antigen/biosynthesis [MESH] |Antineoplastic Agents/chemical synthesis/chemistry/*pharmacology [MESH] |Benzimidazoles/chemical synthesis/chemistry/*pharmacology [MESH] |Cell Line, Tumor [MESH] |Cell Proliferation/drug effects [MESH] |Crystallography, X-Ray [MESH] |Dose-Response Relationship, Drug [MESH] |Drug Screening Assays, Antitumor [MESH] |Humans [MESH] |Models, Molecular [MESH] |Molecular Structure [MESH] |Neoplastic Stem Cells/*drug effects [MESH] |Structure-Activity Relationship [MESH]Cancer stem cells CD133 inhibition and cytotoxicity of certain 3-phe(epmc).pdf DeepDyve Pubget Overpricing