Synthesis of some A- and D-ring fused steroidal pyrazoles, isoxazoles and pyrimidines

N‐substituted Piperazinopyridylsteroid Derivatives as Abiraterone Analogues Inhibit Growth and Induce Pro‐apoptosis in Human Hormone‐independent Prostate Cancer Cell Lines

“…Among these heterocycle steroids, natural steroids contain one or more heterocyclic ring(s), fused or attached to A or D ring, and or formed by modifications of the side chain, which are sufficiently plentiful to become major sources of steroidal intermediates for the synthesis of steroid hormones and pharmaceutical analogues, and furostans , as well as steroidal alkaloids , all have received much attention in view of their relevant biological activities. Considerable effort has been made during the past decade to develop steroidal moiety with pyrazole, isoxazole, pyridine, dehydropiperazine, pyran, pyrrole, or pyrimidine rings using various synthetic strategies . A large number of steroid derivatives bearing modifications in ring D with nitrogen coupled to heterocycles such as imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidyl, oxazinyl and tetrahydro‐oxazinyl heterocycles are efficient inhibitors of cytochrome P450 enzymes and exhibit promising effects as potential agents in the treatment of patients with androgen‐dependent diseases .…”

A new and facile synthetic approach to substituted 2-thioxoquinazolin-4-ones by the annulation of a pyrimidine derivative

“…Recently, we reported the synthesis of fused heterocycles from ethoxymethylene derivatives of DTBA [27]. In continuation of our work on the synthesis of fused heterocycles [28–29], we herein report full details of the work and studies related to the synthesis of 2-thioxoquinazolin-4-ones from the reaction of ethoxymethylene derivatives of DTBA and active methylene compounds, such as, malononitrile and ethylcyanoacetate.…”

Synthesis of Steroidal D‐Ring‐Fused Pyrrolidines of Dehydroepiandrosterone

“…Steroids fused through the D ‐ring to various types of heterocycles, including pyridines, pyrimidines, pyridazines, thiazoles, imidazoles,[1b] pyrazoles, indoles, and polyheterocyles,, have become part of a growing research field. Members of this class of compounds, which are based on the combination of two medicinally relevant privileged core structures into a single molecule, show diverse biological activities.…”