80774-13-6Relevant academic research and scientific papers
Synthesis of imidazothiadiazole-benzimidazole conjugates as mitochondrial apoptosis inducers
Kamal, Ahmed,Ponnampalli, Swapna,Vishnuvardhan,Rao, M. P. Narasimha,Mullagiri, Kishore,Nayak, V Lakshma,Chandrakant, Bagul
, p. 1644 - 1650 (2014/12/11)
A series of imidazothiadiazole-benzimidazole conjugates (3a-z) were synthesized and evaluated for their cytotoxic activity against a set of four selected human cancer cell lines. Amongst them, compounds 3b and 3y exhibited significant antiproliferative activity in ME-180 (cervical) cell line. Flow cytometric analysis showed that these two compounds arrested the cell cycle in the G0/G1 phase leading to the loss of mitochondrial membrane potential followed by apoptotic cell death. Further, Hoechst 33258 staining, DNA fragmentation assay, Annexin V staining assay and caspase-3 also suggested that 3b and 3y induced cell death by apoptosis. Docking studies revealed that compound 3b binds to the Gly142, Phe101, Asn140 and Arg143 on B-cell lymphoma 2 (Bcl-2) proteins and inhibition of Bcl-2 protein could be the possible mechanism of action for these compounds.
New imidazoazole-alkenoic acid amide compounds, intermediate products for their production, their production, and their medicinal use
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, (2008/06/13)
The invention relates to imidazoazole-alkenoic acid amides of Formula (I) and methods for their production. Also included in the invention are compositions containing said alkenoic acid amides and methods for the use of said alkenoic acid amides and the c
