17-Oxo-17a-Aza-D-Homo-5-Androsten-3β-Yl Esters: Cytotoxic To Liver and Neuroblastoma Cancer Cell Lines

• SK Gorla

  English

  Author

• S Velivelli

  English

  Author

• DK Satpathi

  English

  Author

The activity profile of these compounds is significantly impacted by the introduction and placement of
the heteroatom in the parental steroid skeleton. Numerous biologically significant azasteroids have been
identified as GABA receptor antagonists, neuromuscular blocking drugs, antifungals, antilipemics, local
anesthetics, and antimicrobials. The synthesis and assessment of 17-Oxo-17a-aza-D-homo-5-androsten-
3β-yl ester derivatives as possible 5-alpha reductase inhibitors have been reported in recent work from our
lab. Using additional human cancer cell lines, the current work was conducted to further explore the
cytotoxicity of the newly synthesized derivative. Finasteride, 5-fluorouracil, mitocycin 6, and adriamycin
were employed as reference medications for comparison after seven human cancer cell lines were treated
to 1X 10-5m (single dose) of compounds 1–8. Following labeling with sulforhodamine B dye (SRB),
which binds to basic amino acid residues in the trichloroacetic acid (TCA) fixed cells, the cell proliferation
was assessed using an ELISA reader 24 hours later. Every experiment was run in four duplicates. When
compared to conventional reference medications, the newly synthesized azasteroids derivatives
demonstrated notable cytotoxicity against liver and neuroblastoma cell lines. This suggests that 17a-
azasteroids may have the ability to cause in vitro cytotoxicity, together with previously documented
antiproliferative activity against prostate cancer cell lines (DU-145) and 5-alpha reductase inhibitory
action. The findings of these investigations will serve as a basis for future research into new substances
that can be used as chemotherapeutic agents

• pdf