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Synthesis of Some New Benzimidazole–Thiazole Derivatives as Anticancer Agents
Authors:Zienab M Nofal  Elsyed A Soliman  Somaia S Abd El‐Karim  Magdy I El‐Zahar  Aladdin M Srour  Shalini Sethumadhavan  Timothy J Maher
Institution:1. Therapeutical Chemistry Department, National Research Centre, Dokki, Cairo, Egypt;2. Chemistry Department, Faculty of Science, Ain Shams University, El Abbassia, Cairo, Egypt;3. Massachusetts College of Pharmacy and Health Sciences, Boston, USA
Abstract:4‐(1H‐benzod]imidazol‐2‐yl)thiazol‐2‐amine and its 1‐methyl derivative ( 1 ) were reacted with different reagents such as acid anhydrides, malononitrile, chloroacetyl chloride, and aromatic aldehydes to produce the corresponding benzimidazole products 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , respectively. Also, 2‐chloro‐N‐(4‐(1‐methyl‐1H‐benzod]imidazol‐2‐yl)thiazol‐2‐yl) acetamide ( 6 ) was reacted with diaminoethane, ortho‐substituted aniline, thioglycolic acid, thiosemicarbazide derivatives, secondary amines, and potassium isothiocyanate to afford the corresponding derivatives 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , respectively. The cytotoxic activity of some newly synthesized derivatives was studied against two different cell lines HepG2 and PC12. Compounds 9 and 15b showed promising anticancer activity against both types of the tested cancerous cell lines.
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