DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF STEROIDAL TETRAZOLES AS ANTIPROLIFERATIVE AND ANTIOXIDANT AGENTS

Shams uzzaman, Mohd. Asif, Abad Ali, Ashraf Mashrai, Hena Khanam, Asif Sherwani, Mohammad Owais

Abstract


A series of steroidal tetrazole derivatives (7-9) has been obtained by facile and convenient method in a two-step process. All the newly synthesized compounds were characterized by means of elemental analyses, IR, 1H NMR, 13C NMR and MS. The mean surface roughness value (Ra) of compound 9 was found to be 10.32 measured with AFM. Lipinski’s ‘Rule of Five’ analysis and biological score predicted higher intrinsic quality and revealed that these compounds possess good passive oral absorption. The antiproliferative activity was tested in vitro against HeLa (cervical cancer), KCL-22 (myeloid leukemia), MDA-MBA-231 (breast cancer) and normal cell lines, PBMCs (blood peripheral mononuclear) by MTT assay. The synthesized compounds exhibited moderate to good activity against the three human cancer cell lines and were found to be nontoxic to the normal cell lines. In addition, the synthesized compounds were tested for their in vitro antioxidant activity by DPPH method in which compound 9 exhibited good antioxidant activity. 


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DOI: http://dx.doi.org/10.17628/ecb.2014.3.1075-1080

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