106833-39-0Relevant academic research and scientific papers
Reinvestigation of 1,3,4-thiadiazol-2(3h)-iminium bromide in the two-step synthesis of imidazo[2,1-b][1,3,4]- thiadiazoles
Sano, Shigeki,Matsuura, Keisuke,Sumiyoshi, Hayato,Miki, Akira,Kitaike, Syuji,Nakao, Michiyasu
, p. 1041 - 1053 (2014/04/17)
The synthesis of 1,3,4-thiadiazol-2(3H)-iminium bromides, which are intermediates in the most commonly used synthetic approach to imidazo[2,1-b][1,3,4]thiadiazoles, and a single crystal X-ray diffraction study of one of these iminium bromides are describe
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
supporting information, 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.
