Matches in SemOpenAlex for { <https://semopenalex.org/work/W2891908045> ?p ?o ?g. }
- W2891908045 endingPage "83" @default.
- W2891908045 startingPage "73" @default.
- W2891908045 abstract "In this study, synthesis, structural characterization, molecular docking studies, and antiproliferative effects in four different cell lines of several novel 16-arylidene-4-azaandrost-5-ene compounds are reported. These compounds were prepared by oxidative cleavage of the enone system of androstenedione followed by an azacyclization reaction and an aldol condensation with various aldehydes at C16. In the androgen-dependent LNCaP cells, the most relevant antiproliferative effects were observed with the 16-phenyl, 16-p-tolyl, and 16-p-nitrophenyl derivatives. Compound 16E-[(4-methylphenyl)methylidene]-4-azaandrost-5-ene-3,17-dione was the most potent in these cells (IC50 = 28.28 μM), having lower antiproliferative effects in the androgen-independent PC-3 cells (IC50 = 45.31 μM). In addition, an interesting selectivity toward cancer cell lines was found for all compounds because a generally low cytotoxicity was detected in healthy human fibroblasts. Furthermore, the 16-p-tolylazaandrostene steroid induced a reduction of viability in LNCaP cells similar to that observed with finasteride, a clinically used 5α-reductase inhibitor. Moreover, molecular docking studies predicted that these 4-azaandrostene derivatives can interact with 5β-reductase, which has a high level of similarity to 5α-reductase enzyme, and with other common targets of steroidal drugs, particularly the enzyme 17α-hydroxylase/17,20-lyase." @default.
- W2891908045 created "2018-09-27" @default.
- W2891908045 creator A5001591241 @default.
- W2891908045 creator A5062327376 @default.
- W2891908045 creator A5063556772 @default.
- W2891908045 creator A5090227152 @default.
- W2891908045 date "2019-01-01" @default.
- W2891908045 modified "2023-10-02" @default.
- W2891908045 title "Novel 4-azaandrostenes as prostate cancer cell growth inhibitors: Synthesis, antiproliferative effects, and molecular docking studies" @default.
- W2891908045 cites W1558621919 @default.
- W2891908045 cites W1739267297 @default.
- W2891908045 cites W1860446288 @default.
- W2891908045 cites W1966337486 @default.
- W2891908045 cites W1966975021 @default.
- W2891908045 cites W1982861164 @default.
- W2891908045 cites W1984328540 @default.
- W2891908045 cites W1987017002 @default.
- W2891908045 cites W2003778789 @default.
- W2891908045 cites W2009238389 @default.
- W2891908045 cites W2010007086 @default.
- W2891908045 cites W2010587415 @default.
- W2891908045 cites W2010888028 @default.
- W2891908045 cites W2015486391 @default.
- W2891908045 cites W2019269074 @default.
- W2891908045 cites W2021424019 @default.
- W2891908045 cites W2032411451 @default.
- W2891908045 cites W2037242231 @default.
- W2891908045 cites W2041646007 @default.
- W2891908045 cites W2052937370 @default.
- W2891908045 cites W2055585711 @default.
- W2891908045 cites W2057472328 @default.
- W2891908045 cites W2059111185 @default.
- W2891908045 cites W2069529762 @default.
- W2891908045 cites W2070955057 @default.
- W2891908045 cites W2074514308 @default.
- W2891908045 cites W2086501038 @default.
- W2891908045 cites W2105668062 @default.
- W2891908045 cites W2120484554 @default.
- W2891908045 cites W2142404884 @default.
- W2891908045 cites W2157715384 @default.
- W2891908045 cites W2158534713 @default.
- W2891908045 cites W2169574191 @default.
- W2891908045 cites W2206304724 @default.
- W2891908045 cites W2235523093 @default.
- W2891908045 cites W2410817546 @default.
- W2891908045 cites W2419467856 @default.
- W2891908045 cites W2622523929 @default.
- W2891908045 cites W2768770475 @default.
- W2891908045 cites W2792999173 @default.
- W2891908045 doi "https://doi.org/10.1016/j.crci.2018.07.011" @default.
- W2891908045 hasPublicationYear "2019" @default.
- W2891908045 type Work @default.
- W2891908045 sameAs 2891908045 @default.
- W2891908045 citedByCount "9" @default.
- W2891908045 countsByYear W28919080452019 @default.
- W2891908045 countsByYear W28919080452020 @default.
- W2891908045 countsByYear W28919080452021 @default.
- W2891908045 countsByYear W28919080452022 @default.
- W2891908045 countsByYear W28919080452023 @default.
- W2891908045 crossrefType "journal-article" @default.
- W2891908045 hasAuthorship W2891908045A5001591241 @default.
- W2891908045 hasAuthorship W2891908045A5062327376 @default.
- W2891908045 hasAuthorship W2891908045A5063556772 @default.
- W2891908045 hasAuthorship W2891908045A5090227152 @default.
- W2891908045 hasConcept C109316439 @default.
- W2891908045 hasConcept C121608353 @default.
- W2891908045 hasConcept C134651460 @default.
- W2891908045 hasConcept C159110408 @default.
- W2891908045 hasConcept C181199279 @default.
- W2891908045 hasConcept C185592680 @default.
- W2891908045 hasConcept C190283241 @default.
- W2891908045 hasConcept C202751555 @default.
- W2891908045 hasConcept C2775874879 @default.
- W2891908045 hasConcept C2776235491 @default.
- W2891908045 hasConcept C2777486698 @default.
- W2891908045 hasConcept C2779723316 @default.
- W2891908045 hasConcept C41685203 @default.
- W2891908045 hasConcept C53227056 @default.
- W2891908045 hasConcept C54355233 @default.
- W2891908045 hasConcept C55493867 @default.
- W2891908045 hasConcept C62112901 @default.
- W2891908045 hasConcept C71240020 @default.
- W2891908045 hasConcept C71924100 @default.
- W2891908045 hasConcept C86803240 @default.
- W2891908045 hasConcept C96232424 @default.
- W2891908045 hasConceptScore W2891908045C109316439 @default.
- W2891908045 hasConceptScore W2891908045C121608353 @default.
- W2891908045 hasConceptScore W2891908045C134651460 @default.
- W2891908045 hasConceptScore W2891908045C159110408 @default.
- W2891908045 hasConceptScore W2891908045C181199279 @default.
- W2891908045 hasConceptScore W2891908045C185592680 @default.
- W2891908045 hasConceptScore W2891908045C190283241 @default.
- W2891908045 hasConceptScore W2891908045C202751555 @default.
- W2891908045 hasConceptScore W2891908045C2775874879 @default.
- W2891908045 hasConceptScore W2891908045C2776235491 @default.
- W2891908045 hasConceptScore W2891908045C2777486698 @default.
- W2891908045 hasConceptScore W2891908045C2779723316 @default.
- W2891908045 hasConceptScore W2891908045C41685203 @default.