DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF
STEROIDAL TETRAZOLES AS ANTIPROLIFERATIVE AND
ANTIOXIDANT AGENTS
Shamsuzzaman, 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, blood peripheral
mononuclear (PBMC) 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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