Biomedicine

Abstract

Introduction and Aim: Synthesis of antineoplastic drugs is challenging and shrouded with possibilities of multidrug resistance and numerous side effects. Imidazo[2,1-b] [1,3,4] thiadiazole moieties exhibit tremendous scope as novel anti-cancer molecules. In the present study, we synthesize and characterize a series of 5(a-e) Imidazo [2, l-b] [1, 3,4]thiadiazole derivatives and evaluate them for antiproliferative properties using in vivo, in vitro , and in silico approach.
Materials and Methods: The in vivo studies conducted using murine Ehrlich Ascites Cancer (EAC) cell model establishes that treatment with 5c reduces the tumorigenesis by promoting apoptosis in EAC-bearing mice. The cells retrieved from the control and treatment arms of EAC cell bearing mice were used for nuclear and Giemsa staining, DNA fragmentation, RT-PCR and chorioallantoic membrane evaluations.
Results: 5c induces apoptosis, plasma membrane degradation, up-regulation of apoptotic genes and anti-angiogenic characteristics. In vitro evaluation of 5c using, various cancer cell lines against normal fibroblast 3T3 L1 cells confirm 5c sensitivity to MCF-7 with IC50 value of 8μM. 5c exudes marked reduction in cell viability, dual nuclear staining, and long-term colony formation assays in these cells.
Conclusion: 5c inhibits the growth and proliferation of cancer cells. The results of our molecular docking predictions further substantiate our claim. This study is valuable as 5c exhibits a promising approach for the treatment of cancer and its anti-proliferative potential can be exploited for designing novel anticancer drugs in the near future.