Intramolecular approach to some new D-ring-fused steroidal isoxazolidines by 1,3-dipolar cycloaddition: synthesis, theoretical and in vitro pharmacological studies

Determination of 17α-hydroxylase-C17,20-lyase (P45017α) enzyme activities and their inhibition by selected steroidal picolyl and picolinylidene compounds

“…the newly developed technique bears numerous advantages compared to our earlier radiosubstrate methodologies [13,[37][38]. new procedures use small volume incubates, and apply simple and efficient isolation techniques making these methods suitable for rapid and cost effective estimation of 17-hydroxylase and C 17,20 -lyase activities and their inhibition by test substances.…”

Luxury of N‐Tosylhydrazones in Transition‐Metal‐Free Transformations

“…[53] Inspired by Franksa pproach, [54] they have adopted BF 3 ·Et 2 O-mediated strategyw hich readilyf urnished the bioactive 3,4-dihydrobenzopyrano[3,4-c]pyrazoles 112 in very good yields.S imilarly, O-propargyl salicylaldehydesa nd N-propargyl-2-aminobenzaldehydes were utilized as suitable substratesf or the synthesis of pyrazole-fused dihydrochromenes and dihydroquinolines,respectively,inaone-pot fashion. [53] Inspired by Franksa pproach, [54] they have adopted BF 3 ·Et 2 O-mediated strategyw hich readilyf urnished the bioactive 3,4-dihydrobenzopyrano[3,4-c]pyrazoles 112 in very good yields.S imilarly, O-propargyl salicylaldehydesa nd N-propargyl-2-aminobenzaldehydes were utilized as suitable substratesf or the synthesis of pyrazole-fused dihydrochromenes and dihydroquinolines,respectively,inaone-pot fashion.…”

Synthesis of novel steroidal 16-spiroisoxazolines by 1,3-dipolar cycloaddition, and an evaluation of their antiproliferative activities in vitro

“…Since a number of compounds of spiroisoxazoline type have been reported to exert noteworthy antiproliferative activities [40][41][42] and some steroidal derivatives containing similar heterocyclic moieties have also been demonstrated to inhibit cell proliferation [26,29,32], the newly synthetized isoxazolines (7a-e, 8a-d, 11a-e, 12a-e) were subjected to in vitro pharmacological studies of their cytotoxic effects on three malignant human adherent cell lines, HeLa, MCF7, and A431 (Table 2). Their antiproliferative activities were determined by a microplate-based MTT colorimetric assay [43], in comparison with cisplatin as reference agent.…”

“…As a continuation of our work for the construction of heterocyclic steroids possessing cell-growth inhibitory effect [29][30][31][32], we decided to prepare novel 16-spiroisoxazolinyl androst-5-ene derivatives from an α,β-unsaturated steroidal 17-ketone via 1,3-dipolar cycloaddition. Our goal was to investigate the regio-and stereoselectivity of the process and the influence of steric and electronic factors on the ringclosure reactions.…”