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Deprecated: Implicit conversion from float 296.79999999999995 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 J+Enzyme+Inhib+Med+Chem 2017 ; 32 (1): 986-91 Nephropedia Template TP
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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 #MMPMID28726519
J Enzyme Inhib Med Chem 2017[]; 32 (1): 986-91 PMID28726519show 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 (IC50?=?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 (IC50?=?21 and 29??M, respectively) and MDA-MB-468 (IC50?=?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.