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Rahul Kumar Saini
Nitin Sharma
Tirushi Gupta
Smriti
Keywords:
Aza-steroids; D-homoandrostene; nitrogen-containing steroids; steroid synthesis; ring expansion; 17-aza steroids; heterocyclic steroids; medicinal chemistry
Abstract:
Steroids that contain nitrogen atoms are referred to as aza-steroids; this category of bioactive molecules is an important group with many therapeutic uses (anticancer and enzyme inhibitors). Of the many different types, aza-D-homo-androstene systems have been of particular interest due to the modification of the D-ring of the steroid by replacing carbon atoms in the ring with nitrogen atoms and/or expanding the D-ring and these modifications increased their biological activity and receptor selectivity. In this article, we will review methods developed to make aza-D-homoandrostene derivatives. The methods discussed include the transformation of 17-keto steroids, techniques for expanding the rings, cyclization methods, and including a heterocycle. We will also discuss some of the current synthetic techniques, including Nazarov-type cyclization, aza-diels-alder reactions, and functionalization at C-17. These aza-D-homoandrostene derivatives have demonstrated biological activity as 5 alpha-reductase inhibitors, antiandrogens, and anticancer agents. This article discusses their biological activity and summarizes recent advances and future directions for nitrogen-containing steroidal frameworks..
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International Journal of Recent Research and Review
ISSN: 2277-8322
Vol. XIX, Issue 2
June 2026
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PUBLISHED
June 2026
ISSUE
Vol. XIX, Issue 2
SECTION
Articles
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