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Article: Enzymatic synthesis and bioactivity of estradiol derivative conjugates with different amino acids
Title | Enzymatic synthesis and bioactivity of estradiol derivative conjugates with different amino acids |
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Authors | |
Keywords | Chemoselectivity Conjugate Enzymatic Synthesis Estrogen Receptor Steroids |
Issue Date | 2005 |
Publisher | Pergamon. The Journal's web site is located at http://www.elsevier.com/locate/tet |
Citation | Tetrahedron, 2005, v. 61 n. 24, p. 5933-5941 How to Cite? |
Abstract | A series of N-protected amino acid-estradiol derivative conjugates have been synthesized by coupling of 17β-aminoestra-1,3,5 (10)-trien-3-ol (1) or 17β-hydrazonoestra-1,3,5 (10)-trien-3-ol (2) with different amino acids via the catalysis of subtilisin Carlsberg in organic solvent. Various factors, including the structure of amino acid residue, different N-protecting groups of amino acids, different esters of carboxyl group and water content of the reaction media that influence the efficiency of enzymatic reactions were systematically studied. In vitro biological activity studies revealed that the binding interactions between estradiol derivative conjugates and estrogen receptor can be affected by the properties of the conjugated amino acid, but the effects of the change in binding properties did not result in changes in biological activities in both MCF-7 and HeLa cell lines. © 2005 Elsevier Ltd. All rights reserved. |
Persistent Identifier | http://hdl.handle.net/10722/178884 |
ISSN | 2023 Impact Factor: 2.1 2023 SCImago Journal Rankings: 0.406 |
ISI Accession Number ID | |
References |
DC Field | Value | Language |
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dc.contributor.author | Yan, AX | en_US |
dc.contributor.author | Chan, RYK | en_US |
dc.contributor.author | Lau, WS | en_US |
dc.contributor.author | Lee, KS | en_US |
dc.contributor.author | Wong, MS | en_US |
dc.contributor.author | Xing, GW | en_US |
dc.contributor.author | Tian, GL | en_US |
dc.contributor.author | Ye, YH | en_US |
dc.date.accessioned | 2012-12-19T09:50:24Z | - |
dc.date.available | 2012-12-19T09:50:24Z | - |
dc.date.issued | 2005 | en_US |
dc.identifier.citation | Tetrahedron, 2005, v. 61 n. 24, p. 5933-5941 | en_US |
dc.identifier.issn | 0040-4020 | en_US |
dc.identifier.uri | http://hdl.handle.net/10722/178884 | - |
dc.description.abstract | A series of N-protected amino acid-estradiol derivative conjugates have been synthesized by coupling of 17β-aminoestra-1,3,5 (10)-trien-3-ol (1) or 17β-hydrazonoestra-1,3,5 (10)-trien-3-ol (2) with different amino acids via the catalysis of subtilisin Carlsberg in organic solvent. Various factors, including the structure of amino acid residue, different N-protecting groups of amino acids, different esters of carboxyl group and water content of the reaction media that influence the efficiency of enzymatic reactions were systematically studied. In vitro biological activity studies revealed that the binding interactions between estradiol derivative conjugates and estrogen receptor can be affected by the properties of the conjugated amino acid, but the effects of the change in binding properties did not result in changes in biological activities in both MCF-7 and HeLa cell lines. © 2005 Elsevier Ltd. All rights reserved. | en_US |
dc.language | eng | en_US |
dc.publisher | Pergamon. The Journal's web site is located at http://www.elsevier.com/locate/tet | en_US |
dc.relation.ispartof | Tetrahedron | en_US |
dc.subject | Chemoselectivity | en_US |
dc.subject | Conjugate | en_US |
dc.subject | Enzymatic Synthesis | en_US |
dc.subject | Estrogen Receptor | en_US |
dc.subject | Steroids | en_US |
dc.title | Enzymatic synthesis and bioactivity of estradiol derivative conjugates with different amino acids | en_US |
dc.type | Article | en_US |
dc.identifier.email | Yan, AX: ayan8@hku.hk | en_US |
dc.identifier.authority | Yan, AX=rp00823 | en_US |
dc.description.nature | link_to_subscribed_fulltext | en_US |
dc.identifier.doi | 10.1016/j.tet.2005.02.090 | en_US |
dc.identifier.scopus | eid_2-s2.0-19744364985 | en_US |
dc.relation.references | http://www.scopus.com/mlt/select.url?eid=2-s2.0-19744364985&selection=ref&src=s&origin=recordpage | en_US |
dc.identifier.volume | 61 | en_US |
dc.identifier.issue | 24 | en_US |
dc.identifier.spage | 5933 | en_US |
dc.identifier.epage | 5941 | en_US |
dc.identifier.isi | WOS:000229671600027 | - |
dc.publisher.place | United Kingdom | en_US |
dc.identifier.scopusauthorid | Yan, AX=8621667000 | en_US |
dc.identifier.scopusauthorid | Chan, RYK=22233369800 | en_US |
dc.identifier.scopusauthorid | Lau, WS=7402933267 | en_US |
dc.identifier.scopusauthorid | Lee, KS=7501499950 | en_US |
dc.identifier.scopusauthorid | Wong, MS=23394345200 | en_US |
dc.identifier.scopusauthorid | Xing, GW=7103115645 | en_US |
dc.identifier.scopusauthorid | Tian, GL=7202950710 | en_US |
dc.identifier.scopusauthorid | Ye, YH=7401627480 | en_US |
dc.identifier.issnl | 0040-4020 | - |