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Sara T Al-Rashood

Associate Professor

أستاذ مشارك

كلية الصيدلة
مكتب رقم 76الدورالثاني كليه الصيدله مبنى 8 - المدينه الجامعية للطالبات
publication
Journal Article
2017

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. Journal of Enzyme Inhibition and Medicinal Chemistry

AlRashood,, Ghada H. Al-Ansary, Wagdy M. Eldehna, Hazem A. Ghabbour, Sara T. A. . 2017

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 μM, 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 μM, respectively) and MDA-MB-468 (IC50 = 23 and 24 μM, 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.

Keywords: Cancer stem cellsCD133cytotoxicitycolon cancerbenzimidazolesX-ray

Volume Number
32
Issue Number
1
Magazine \ Newspaper
Journal of Enzyme Inhibition and Medicinal Chemistry
more of publication
publications

Cancer stem cells (CSCs) have been objects of intensive study since their identification in 1994.

by Ghada H. Al-Ansary, Wagdy M. Eldehna, Hazem A. Ghabbour, Sara T. A. AlRashood,
2017
publications

A series of amide chalcones conjugated with different secondary amines were synthesised and characterised by different spectroscopic techniques 1H NMR, 13C NMR, and ESI-MS. They were screened for…

by Shahenda M. El-Messery, El-Sayed E. Habib, Sarah T. A. Al-Rashood & Ghada
2018
publications

مرادفات الثياديازولودايزبين - طرق تحضيرها - تركيباتها و فاعليتها كعلاج مبتكر لمرض الصرع

2017