Výsledky vyhledávání - "C17 20 lyase"

Synthesis of 16α-amino-pregnenolone derivatives via ionic liquid-catalyzed aza-Michael addition and their evaluation as C17,20-lyase inhibitors

Autor: Johan Wouters, Mihály Szécsi, Rita Skoda-Földes, Gábor Mikle, Lilla Maksó, László Kollár, Bianka Edina Herman, Eszter Szánti-Pintér, Ágnes Gömöry

Publikováno v: Steroids. 123:61-66

Aza-Michael addition of 16-dehydropregnenolone was studied in the presence of a basic ionic liquid, [DBU][OAc] as catalyst and solvent. The reaction was carried out using different primary and secondary amines as N-nucleophiles. The products were obt

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4405391a033cfb6d53518ce6bf03e7c
https://doi.org/10.1016/j.steroids.2017.05.006

Zobrazit plný text záznamu

An efficient approach to novel 17-5′-(1′,2′,4′)-oxadiazolyl androstenes via the cyclodehydration of cytotoxic O-steroidacylamidoximes, and an evaluation of their inhibitory action on 17α-hydroxylase/C17,20-lyase

Autor: János Wölfling, Mihály Szécsi, Dóra Kovács, Éva Frank, Ida Kovács, István Zupkó, Nikoletta Szabó

Publikováno v: European Journal of Medicinal Chemistry. 70:649-660

Novel 17-exo-oxadiazoles in the androst-5-ene series were efficiently synthesized in a two-step sequence via the corresponding O-acylamidoxime intermediates (obtained from steroidal 17-carboxylic acids and amidoximes in the presence of coupling reage

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::24a48546e8d98e950c7572b6111ad380
https://doi.org/10.1016/j.ejmech.2013.10.038

Zobrazit plný text záznamu

Synthetic studies on (1S)-1-(6,7-dimethoxy-2-naphthyl)-1-(1H-imidazol-4-yl)-2-methylpropan-1-ol as a selective C17,20-lyase inhibitor

Autor: Nobuyuki Matsunaga, Akio Ojida, Akihiro Tasaka, Tomohiro Kaku

Publikováno v: Tetrahedron: Asymmetry. 15:2021-2028

An asymmetric synthesis of the selective C 17,20 -lyase inhibitor 2 has been established in eight steps from 2,3-dihydroxynaphthalene 9 . The key steps are the enantioselective oxidation of ketone 17 to the chiral α-hydroxy ketone 18 and the diaster

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6a8e1e04a65d4c83d24d0697e3c71260
https://doi.org/10.1016/j.tetasy.2004.05.044

Zobrazit plný text záznamu

Stereocontrolled synthesis of (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methylpropan-1-ol as a potent C17,20-lyase inhibitor

Autor: Akio Ojida, Akihiro Tasaka, Nobuyuki Matsunaga, Tomohiro Kaku

Publikováno v: Tetrahedron: Asymmetry. 15:1555-1559

An efficient stereocontrolled synthesis of the potent C17,20-lyase inhibitor, (1S)-1-(1H-imidazol-4-yl)-1-(6-methoxy-2-naphthyl)-2-methyl-1-propanol 1, has been established. The stereogenic center of 1 was successfully constructed by a highly diaster

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::40bfc74f8b2d313ed966c6fbb27b7d38
https://doi.org/10.1016/j.tetasy.2004.02.035

Zobrazit plný text záznamu

C16 and C17 Substituted Derivatives of Pregnenolone and Progesterone as Inhibitors of 17α-Hydroxylase-C17, 20-lyase: Synthesis and Biological Evaluation

Autor: Rolf W. Hartmann, Samer Haidar

Publikováno v: Archiv der Pharmazie. 335:526-534

17 alpha-hydroxylase-C17, 20-lyase (P450 17, CYP 17) is a key enzyme in androgen biosynthesis and a target for the treatment of prostate cancer. In order to find novel inhibitors for this enzyme, several compounds bearing different moieties able to c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7cfc7da3870b61bf7fdf154380a52660
https://doi.org/10.1002/ardp.200290006

Zobrazit plný text záznamu

Inhibition of steroid C17(20) lyase with C-17-heteroaryl steroids

Autor: Norton P. Peet, Robert J. Resvick, Joseph P. Burkhart, Cynthia A. Gates, Marie E. Laughlin

Publikováno v: Bioorganic & Medicinal Chemistry. 4:1411-1420

Steroids bearing a heteroaromatic substituent at C-17 were designed as inhibitors of C 17(20) lyase. The thiazoles, furans, and thiophenes appended to the steroid nucleus were positioned on the α-face and the β-face of the steroid, and conjugated w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93dc29c758106655c2facabdcbfc4592
https://doi.org/10.1016/0968-0896(96)00135-6

Zobrazit plný text záznamu

Time-dependent inactivation of steroid C17(20) lyase by 17β-cyclopropyl ether-substituted steroids

Autor: Angela L. Marquart, Marie E. Laughlin, Norton P. Peet, Cynthia A. Gates, Thomas R. Blohm, Philip M. Weintraub, Michael R. Angelastro

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:97-100

Androstenes bearing a cyclopropyl group attached to the C-17β position with a heteroatom linker, designed as mechanism-based inhibitors of steroid C 17(20) lyase, were found to be potent, time-dependent inhibitors of this enzyme.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7ea2b3228e504186ef90e7958913109b
https://doi.org/10.1016/0960-894x(95)00566-c

Zobrazit plný text záznamu

Active-site conformation of 17-(3-pyridyl)androsta-5,16-dien-3β-ol, a potent inhibitor of the P450 enzyme C17α-hydroxylase/C17-20 lyase

Autor: Charles A. Laughton, C. F. Snook, David F. Burke, Michael Jarman, Gerard A. Potter, Stephen Neidle

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:1125-1130

17-(3-pyridyl)androsta-5,16-dien-3β-ol, a nanomolar inhibitor of the P450 enzyme C17α-hydroxylase/C17-20 lyase, is a target for prostate cancer chemotherapy. A model is presented for the inhibitor docked into the structure of the enzyme.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cacba9c6c5b9e343c786114385eaf0e3
https://doi.org/10.1016/0960-894x(95)00178-v

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání