Synthesis and antineoplastic activity of O-alkylated derivatives of 7-hydroximinoandrost-5-ene steroids.

Arch Pharm (Weinheim)

University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh, India.

Published: July 2010

AI Article Synopsis

  • The positioning of the hydroximino group on steroid compounds significantly alters their effectiveness against cancer.
  • Researchers synthesized and tested 7-oximino-5-androstene and its derivatives for their ability to kill cancer cells and inhibit aromatase.
  • While the steroidal 7-oximino derivatives showed little cytotoxicity against various cancer cell lines, the imidazolyl-substituted versions demonstrated some inhibition of cytochrome P450 aromatase activity.

Article Abstract

Varied positioning of the hydroximino group on the parental steroid skeleton results in remarkable changes in the antineoplastic activity profile of the compounds. Here, the compound 7-oximino-5-androstene and its O-alkylated derivatives have been prepared and screened for cytotoxic and aromatase inhibitory activity. The steroidal 7-oximino ether derivatives exhibited insignificant cytotoxic effects when screened against three cancer cell lines, MCF-7 (breast), NCl-H460 (lung), and SF-268 (CNS) at 100 microM. However, the imidazolyl-substituted steroidal oxime ethers displayed moderate inhibition of cytochrome P450 aromatase.

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Source
http://dx.doi.org/10.1002/ardp.200900258DOI Listing

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