Vol.:(0123456789) 1 3 Cancer Chemother Pharmacol DOI 10.1007/s00280-017-3414-6 SHORT COMMUNICATION Inhibitory growth evaluation and apoptosis induction in MCF‑7 cancer cells by new 5‑aryl‑2‑butylthio‑1,3,4‑oxadiazole derivatives Rashmin Khanam 1  · Kamal Ahmad 1  · Iram I. Hejazi 1  · Ibrar A. Siddique 2  · Vikash Kumar 2  · Abdul Roouf Bhat 3  · Amir Azam 4  · Fareeda Athar 1   Received: 14 March 2017 / Accepted: 3 August 2017 © Springer-Verlag GmbH Germany 2017 involved in the attainment of cellular immortality and carcinogenesis. Result In vitro MTT screening assay showed the com- pound 5-aminophenyl-2-butylthio-1,3,4-oxadiazole (5e) showing the highest inhibitory efect against MCF-7 cancer cell with IC 50 value 10.05 ± 1.08 µM while it is much safer and less toxic on normal cell line (HEK-293). The dose- dependent treatment of MCF-7 cells with 5e resulted in inhibition of cell migration in the wound healing assay. The fow-cytometry analysis showed the cells arrested in G0/ G1 phase of the cell cycle. Compound 5e induced apopto- sis of MCF-7 cells was characterized using DAPI staining and Annexin V-PE/7-AAD dual binding assay. Reduction of NBT by compound 5e showed a reduced generation of ROS. Western blotting studies showed high activation of apoptotic protein Caspase3 and decrease in expression of anti-apoptotic protein BCL-2. Conclusion Based on the results of in vitro studies, it could be concluded that compound 5e showed a signifcant inhibi- tory growth efect on MCF-7 cells and have the potential to be developed as lead molecule and further structural modif- cations may result in promising new anticancer agents. Abstract Background Cancer has become one of the global health issues and it is the life-threatening disease characterized by unrestrained growth of cells. Despite various advances being adopted by chemotherapeutic management, the use of the current anticancer drugs such as Doxorubicin, Asparginase, Methotrexate, Vincristine remains limited due to high tox- icity, side efects and developing drug resistance. Apopto- sis is a crucial cellular process and improper regulation of apoptotic signaling pathways may lead to cancer formation. Subsequently, the synthesis of efective chemotherapeutic agents that can induce apoptosis in tumor cell has emerged as a signifcant approach in cancer drug discovery. Methods The goal of this work is to develop a potential antitumor agent exerting signifcant inhibitory efects on cancer cell and low cytotoxicity, for which we focused on the structural features of 1,3,4-oxadiazoles as it a privileged scafold in modern medicinal chemistry and have the ability to inhibit growth factors, enzymes and kinases potentially Electronic supplementary material The online version of this article (doi:10.1007/s00280-017-3414-6) contains supplementary material, which is available to authorized users. * Abdul Roouf Bhat abroouf@gmail.com * Fareeda Athar fathar@jmi.ac.in 1 Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi 110025, India 2 National Institute of Immunology, New Delhi 110067, India 3 Department of Chemistry, Sri Pratap College, Cluster University, Srinagar 190001, India 4 Department of Chemistry, Jamia Millia Islamia, New Delhi 110025, India