Synthesis and Antineoplastic Activity of O‐Alkylated Derivatives of 7‐Hydroximinoandrost‐5‐ene Steroids |
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| Authors: | Ranju Bansal Sheetal Guleria Christina Ries Rolf W. Hartmann |
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| Affiliation: | 1. University Institute of Pharmaceutical Sciences, Sector‐14, Panjab University, Chandigarh, India. Fax: +91 172 254‐1142;2. Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbrücken, Germany |
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| 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 μM. However, the imidazolyl‐substituted steroidal oxime ethers displayed moderate inhibition of cytochrome P450 aromatase. |
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| Keywords: | Antineoplastic activity Aromatase inhibitory activity Hydroximino steroids Oxime ethers |
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