752244-20-5Relevant academic research and scientific papers
Design and synthesis of imidazo[2,1-b]thiazole linked triazole conjugates: Microtubule-destabilizing agents
Shaik, Siddiq Pasha,Nayak, V. Lakshma,Sultana, Faria,Rao, A.V. Subba,Shaik, Anver Basha,Babu, Korrapati Suresh,Kamal, Ahmed
, p. 36 - 51 (2016/10/25)
A series of imidazo[2,1-b]thiazole linked triazole conjugates were synthesized by using Huisgen 1,3-dipolar cyclo-addition reaction (click chemistry approach) and evaluated for their antiproliferative activity against some human cancer cell lines like, HeLa (cervical), DU-145 (prostate), A549 (lung), MCF-7 (breast) and HepG2 (liver). Among them, Conjugates 4g and 4h demonstrated a significant antiproliferative effect against human lung cancer cells (A549) with IC50values of 0.92 and 0.78 μM respectively. Flow cytometric analysis revealed that these conjugates induced cell cycle arrest in G2/M phase in A549 lung cancer cells. The tubulin polymerization assay and immunofluorescence analysis showed that these conjugates effectively inhibit microtubule assembly in cell free and cell based (A549) experiment respectively. Moreover, the apoptosis inducing properties were evaluated by Hoechst staining, mitochondrial membrane potential and Annexin V-FITC assay. Further, western blot analysis was performed for proapoptotic protein Bax and antiapoptotic protein Bcl-2 and the results demonstrated that there was up regulation of Bax and down regulation of Bcl-2 suggesting that these compounds induced apoptosis in human lung cancer cells, A549.
Synthesis of ethyl 8-aryl-8-hydroxy-3-oxo-8H[1,2,4]oxadiazolo-[3,4-c][1,4] thiazine-5-carboxylates by ring-expansion rearrangement
Koti, Rajesh,Hegde, Vinayak,Kolavi, Gundurao,Khazi, Imtiyaz Ahmed
, p. 1715 - 1722 (2008/02/01)
The title compounds were prepared by the ring-ring interconversion of ethyl 5-nitroso-6-arylimidazo[2,1-b]thiazole-3-carboxylates with hydrochloric acid. The effect of electron-withdrawing substituent in the thiazole ring on the general applicability of t
Synthesis and biological activity of some 3-methyl/ethoxycarbonyl-6-arylimidazo[2,1-b]thiazoles and their 5-bromo/ 5-formyl derivatives
Khazi,Koti,Gadad,Mahajanshetti,Shivakumar,Akki
, p. 393 - 398 (2007/10/03)
Facile reaction of arylacylbromide 1 with 2-amino-4-methylthiazole 2 and its hindered reaction with 2-amino-4-ethoxycarbonylthiazole 3 during the synthesis of 3-methyl/ethoxycarbonyl-6-arylimidazo[2,1-b]thiazoles 8/9 are explained on the basis of electron
