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ID: ALA3352503
Journal: Bioorg Med Chem Lett
Title: An investigation of in vitro cytotoxicity and apoptotic potential of aromatic diselenides.
Authors: Rizvi MA, Guru S, Naqvi T, Kumar M, Kumbhar N, Akhoon S, Banday S, Singh SK, Bhushan S, Mustafa Peerzada G, Shah BA.
Abstract: A target synthesis of a library of symmetric aromatic diselenides was attempted with the aim of generating anticancer lead compounds. Out of thirteen screened molecules (1-13) against a panel of human cancer cell lines, compound 8 exhibited highest cell growth inhibition in Human leukemia HL-60 cells with IC50 value of 8 μM. Compound 8 had a good pro-apoptotic potential as evidenced from several apoptotic protocols like DNA cell cycle analysis and monitoring of apoptotic bodies formation using phase contrast and nuclear microscopy with Hoechst 33,258. Also, 8 significantly inhibits S phase of the cell cycle and eventually trigger apoptosis in HL-60 cells through mitochondrial dependent pathway substantiated by the loss of mitochondrial potential. A theoretical investigation of DNA binding ability of 8 showed that it selectively bind to minor groove of DNA, where it is stabilized by hydrogen bonding and hydrophobic interactions.
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