73667-70-6Relevant academic research and scientific papers
Identification of a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain
Iyer, Divyaanka,Vartak, Supriya V.,Srivastava, Mrinal,Hegde, Mahesh,Gopalakrishnan, Vidya,Raghavan, Sathees C.,Mishra, Archita,Surolia, Avadhesha,Goldsmith, Gunaseelan,Velusamy, Mahesh,Choudhary, Bibha,Kumar, Sujeet,Karki, Subhas S.,Glenn, Mark,Kalakonda, Nagesh
, p. 3408 - 3437 (2016/12/31)
The antiapoptotic protein BCL2 is overexpressed in several cancers and contributes to prolonged cell survival and chemoresistance, lending itself as an excellent target for cancer therapy. Here, we report the design, synthesis, and characterization of Dis
Synthesis and antiproliferative activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives
Kumar, Sujeet,Gopalakrishnan, Vidya,Hegde, Mahesh,Rana, Vivek,Dhepe, Sharad S.,Ramareddy, Sureshbabu A.,Leoni, Alberto,Locatelli, Alessandra,Morigi, Rita,Rambaldi, Mirella,Srivastava, Mrinal,Raghavan, Sathees C.,Karki, Subhas S.
, p. 4682 - 4688 (2015/01/09)
A series of 2,5,6-substituted imidazo[2,1-b][1,3,4]thiadiazole derivatives have been prepared and were tested for antiproliferative activity on cancer cells at the National Cancer Institute. Results showed that molecules with a benzyl group at position 2, exhibited an increase in activity for the introduction of a formyl group at the 5 position. The compound 2-benzyl-5-formyl-6-(4-bromophenyl)imidazo[2,1-b][1,3,4]thiadiazole 22 has been chosen for understanding the mechanism of action by various molecular and cellular biology studies. Results obtained from cell cycle evaluation analysis, analysis of mitochondrial membrane potential and Annexin V-FITC by flow cytometric analysis, ROS production and expression of apoptotic and DNA-repair proteins suggested that compound 22 induced cytotoxicity by activating extrinsic pathway of apoptosis, however, without affecting cell cycle progression.
Synthesis, hypoglycaemic, hypolipidemic and pparγ agonist activities of 5-(2-alkyl/aryl-6-arylimidazo[2,1-b][1,3,4]thiadiazol-5-yl)methylene-1,3-thiazolidinediones
Khazi, Mohammed Iqbal A.,Belavagi, Ningaraddi S.,Kim, Kwang R.,Gong, Young-Dae,Khazi, Imtiyaz Ahmed M.
, p. 147 - 155 (2013/08/23)
A novel series of 5-(2-alkyl/aryl-6-arylimidazo[2,1-b][1,3,4]thiadiazol-5-yl)methylene-1,3-thiazolidinediones were synthesized as possible PPARγ agonists. The structures of these target molecules were established by spectral and analytical data. All the n
Microwave-assisted synthesis and antimicrobial activity of some imidazo[2,1-b][1,3,4]thiadiazole derivatives
Dhepe, Sharad,Kumar, Sujeet,Vinayakumar,Ramareddy, Sureshbabu A.,Karki, Subhas S.
, p. 1550 - 1556 (2012/11/07)
A simple and efficient method was developed for the synthesis of 2,6-disubstituted-imidazo[2,1-b][1,3,4] thiadiazoles under microwave (MW) activation using 2-amino-5-substituted-1,3,4-thiadiazoles and appropriate bromo ketones as materials. All reactions
