Loading…
Synthesis and pharmacological evaluation of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety
Background Prostate cancer (PCa) is the most common malignancy in men and in the absence of any effective treatments available. Methods For the development of potential anticancer agents, 24 kinds of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety were synthesized and c...
Saved in:
| Published in: | Pharmacological reports 2020-08, Vol.72 (4), p.1058-1068 |
|---|---|
| Main Authors: | , , , , , , |
| Format: | Article |
| Language: | English |
| Subjects: | |
| Citations: | Items that this one cites Items that cite this one |
| Online Access: | Get full text |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| cited_by | cdi_FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3 |
|---|---|
| cites | cdi_FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3 |
| container_end_page | 1068 |
| container_issue | 4 |
| container_start_page | 1058 |
| container_title | Pharmacological reports |
| container_volume | 72 |
| creator | Chen, Hong Qian, Yuna Jia, Huixia Yu, Yuzhong Zhang, Haibo Shen, Jianliang Zhao, Shanchao |
| description | Background
Prostate cancer (PCa) is the most common malignancy in men and in the absence of any effective treatments available.
Methods
For the development of potential anticancer agents, 24 kinds of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety were synthesized and characterized by using spectroscopic methods. Their pharmacological activities were evaluated against human PCa cell lines (PC-3 and LNCaP) and a
1
-adrenergic receptors (a
1
-ARs; α
1a
, α
1b
, and α
1d
-ARs). The structure–activity relationship of these designed arylpiperazine derivatives was rationally explored and discussed.
Results
Among these derivatives,
3c
,
3d
,
3h
,
3k
,
3o
, and
3s
exhibited the most potent activity against the tested cancer cells, and some derivatives with potent anticancer activities exhibited better a
1
-AR subtype selectivity than others did (selectivity ratio > 10).
Conclusion
This work provided a potential lead compound for the further development of anticancer agents for PCa therapy.
Graphic abstract |
| doi_str_mv | 10.1007/s43440-019-00041-w |
| format | article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_2354150731</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2354150731</sourcerecordid><originalsourceid>FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3</originalsourceid><addsrcrecordid>eNp9kMFu1DAURS0EotOBH2BRecnGxY7tOFlWFS1IlVgAa8uxX2ZcOXZqJ1MNX1-XaVmyeot77pXeQegTo5eMUvWlCC4EJZT1hFIqGHl8gzZN0_dEtp14izZMcUEYE_QMnZdy_8w0XL5HZ7yhomvadoOOP49x2UPxBZvo8Lw3eTI2hbTz1gQMBxNWs_gUcRpxNOOSZu98IIMp4LDJxzD7GbL54yNgB9kfKn2Agm2Ki_HRxx2u-3jIaUrzHmIKeEoeluMH9G40ocDHl7tFv2--_rr-Ru5-3H6_vrojlgu1kHGUSo6CSdewfmiV7cwA1gnZcTb0vJXGKGVVzQGcbVwreglK9qrra7MDvkWfT7tzTg8rlEVPvlgIwURIa9HVSF2nirOKNifU5lRKhlHP2U_1Sc2oflauT8p1Va7_KtePtXTxsr8OE7h_lVfHFeAnoNQo7iDr-7TmWH_-3-wT0xOQlA</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2354150731</pqid></control><display><type>article</type><title>Synthesis and pharmacological evaluation of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety</title><source>Springer Nature</source><creator>Chen, Hong ; Qian, Yuna ; Jia, Huixia ; Yu, Yuzhong ; Zhang, Haibo ; Shen, Jianliang ; Zhao, Shanchao</creator><creatorcontrib>Chen, Hong ; Qian, Yuna ; Jia, Huixia ; Yu, Yuzhong ; Zhang, Haibo ; Shen, Jianliang ; Zhao, Shanchao</creatorcontrib><description>Background
Prostate cancer (PCa) is the most common malignancy in men and in the absence of any effective treatments available.
Methods
For the development of potential anticancer agents, 24 kinds of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety were synthesized and characterized by using spectroscopic methods. Their pharmacological activities were evaluated against human PCa cell lines (PC-3 and LNCaP) and a
1
-adrenergic receptors (a
1
-ARs; α
1a
, α
1b
, and α
1d
-ARs). The structure–activity relationship of these designed arylpiperazine derivatives was rationally explored and discussed.
Results
Among these derivatives,
3c
,
3d
,
3h
,
3k
,
3o
, and
3s
exhibited the most potent activity against the tested cancer cells, and some derivatives with potent anticancer activities exhibited better a
1
-AR subtype selectivity than others did (selectivity ratio > 10).
Conclusion
This work provided a potential lead compound for the further development of anticancer agents for PCa therapy.
Graphic abstract</description><identifier>ISSN: 1734-1140</identifier><identifier>EISSN: 2299-5684</identifier><identifier>DOI: 10.1007/s43440-019-00041-w</identifier><identifier>PMID: 32048266</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Drug Safety and Pharmacovigilance ; Medicine ; Pharmacotherapy ; Pharmacy</subject><ispartof>Pharmacological reports, 2020-08, Vol.72 (4), p.1058-1068</ispartof><rights>Maj Institute of Pharmacology Polish Academy of Sciences 2020</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3</citedby><cites>FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,778,782,27907,27908</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/32048266$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chen, Hong</creatorcontrib><creatorcontrib>Qian, Yuna</creatorcontrib><creatorcontrib>Jia, Huixia</creatorcontrib><creatorcontrib>Yu, Yuzhong</creatorcontrib><creatorcontrib>Zhang, Haibo</creatorcontrib><creatorcontrib>Shen, Jianliang</creatorcontrib><creatorcontrib>Zhao, Shanchao</creatorcontrib><title>Synthesis and pharmacological evaluation of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety</title><title>Pharmacological reports</title><addtitle>Pharmacol. Rep</addtitle><addtitle>Pharmacol Rep</addtitle><description>Background
Prostate cancer (PCa) is the most common malignancy in men and in the absence of any effective treatments available.
Methods
For the development of potential anticancer agents, 24 kinds of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety were synthesized and characterized by using spectroscopic methods. Their pharmacological activities were evaluated against human PCa cell lines (PC-3 and LNCaP) and a
1
-adrenergic receptors (a
1
-ARs; α
1a
, α
1b
, and α
1d
-ARs). The structure–activity relationship of these designed arylpiperazine derivatives was rationally explored and discussed.
Results
Among these derivatives,
3c
,
3d
,
3h
,
3k
,
3o
, and
3s
exhibited the most potent activity against the tested cancer cells, and some derivatives with potent anticancer activities exhibited better a
1
-AR subtype selectivity than others did (selectivity ratio > 10).
Conclusion
This work provided a potential lead compound for the further development of anticancer agents for PCa therapy.
Graphic abstract</description><subject>Drug Safety and Pharmacovigilance</subject><subject>Medicine</subject><subject>Pharmacotherapy</subject><subject>Pharmacy</subject><issn>1734-1140</issn><issn>2299-5684</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><recordid>eNp9kMFu1DAURS0EotOBH2BRecnGxY7tOFlWFS1IlVgAa8uxX2ZcOXZqJ1MNX1-XaVmyeot77pXeQegTo5eMUvWlCC4EJZT1hFIqGHl8gzZN0_dEtp14izZMcUEYE_QMnZdy_8w0XL5HZ7yhomvadoOOP49x2UPxBZvo8Lw3eTI2hbTz1gQMBxNWs_gUcRpxNOOSZu98IIMp4LDJxzD7GbL54yNgB9kfKn2Agm2Ki_HRxx2u-3jIaUrzHmIKeEoeluMH9G40ocDHl7tFv2--_rr-Ru5-3H6_vrojlgu1kHGUSo6CSdewfmiV7cwA1gnZcTb0vJXGKGVVzQGcbVwreglK9qrra7MDvkWfT7tzTg8rlEVPvlgIwURIa9HVSF2nirOKNifU5lRKhlHP2U_1Sc2oflauT8p1Va7_KtePtXTxsr8OE7h_lVfHFeAnoNQo7iDr-7TmWH_-3-wT0xOQlA</recordid><startdate>20200801</startdate><enddate>20200801</enddate><creator>Chen, Hong</creator><creator>Qian, Yuna</creator><creator>Jia, Huixia</creator><creator>Yu, Yuzhong</creator><creator>Zhang, Haibo</creator><creator>Shen, Jianliang</creator><creator>Zhao, Shanchao</creator><general>Springer International Publishing</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20200801</creationdate><title>Synthesis and pharmacological evaluation of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety</title><author>Chen, Hong ; Qian, Yuna ; Jia, Huixia ; Yu, Yuzhong ; Zhang, Haibo ; Shen, Jianliang ; Zhao, Shanchao</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Drug Safety and Pharmacovigilance</topic><topic>Medicine</topic><topic>Pharmacotherapy</topic><topic>Pharmacy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chen, Hong</creatorcontrib><creatorcontrib>Qian, Yuna</creatorcontrib><creatorcontrib>Jia, Huixia</creatorcontrib><creatorcontrib>Yu, Yuzhong</creatorcontrib><creatorcontrib>Zhang, Haibo</creatorcontrib><creatorcontrib>Shen, Jianliang</creatorcontrib><creatorcontrib>Zhao, Shanchao</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmacological reports</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chen, Hong</au><au>Qian, Yuna</au><au>Jia, Huixia</au><au>Yu, Yuzhong</au><au>Zhang, Haibo</au><au>Shen, Jianliang</au><au>Zhao, Shanchao</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and pharmacological evaluation of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety</atitle><jtitle>Pharmacological reports</jtitle><stitle>Pharmacol. Rep</stitle><addtitle>Pharmacol Rep</addtitle><date>2020-08-01</date><risdate>2020</risdate><volume>72</volume><issue>4</issue><spage>1058</spage><epage>1068</epage><pages>1058-1068</pages><issn>1734-1140</issn><eissn>2299-5684</eissn><abstract>Background
Prostate cancer (PCa) is the most common malignancy in men and in the absence of any effective treatments available.
Methods
For the development of potential anticancer agents, 24 kinds of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety were synthesized and characterized by using spectroscopic methods. Their pharmacological activities were evaluated against human PCa cell lines (PC-3 and LNCaP) and a
1
-adrenergic receptors (a
1
-ARs; α
1a
, α
1b
, and α
1d
-ARs). The structure–activity relationship of these designed arylpiperazine derivatives was rationally explored and discussed.
Results
Among these derivatives,
3c
,
3d
,
3h
,
3k
,
3o
, and
3s
exhibited the most potent activity against the tested cancer cells, and some derivatives with potent anticancer activities exhibited better a
1
-AR subtype selectivity than others did (selectivity ratio > 10).
Conclusion
This work provided a potential lead compound for the further development of anticancer agents for PCa therapy.
Graphic abstract</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>32048266</pmid><doi>10.1007/s43440-019-00041-w</doi><tpages>11</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1734-1140 |
| ispartof | Pharmacological reports, 2020-08, Vol.72 (4), p.1058-1068 |
| issn | 1734-1140 2299-5684 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_2354150731 |
| source | Springer Nature |
| subjects | Drug Safety and Pharmacovigilance Medicine Pharmacotherapy Pharmacy |
| title | Synthesis and pharmacological evaluation of naftopidil-based arylpiperazine derivatives containing the bromophenol moiety |
| url | http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-16T22%3A16%3A00IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Synthesis%20and%20pharmacological%20evaluation%20of%20naftopidil-based%20arylpiperazine%20derivatives%20containing%20the%20bromophenol%20moiety&rft.jtitle=Pharmacological%20reports&rft.au=Chen,%20Hong&rft.date=2020-08-01&rft.volume=72&rft.issue=4&rft.spage=1058&rft.epage=1068&rft.pages=1058-1068&rft.issn=1734-1140&rft.eissn=2299-5684&rft_id=info:doi/10.1007/s43440-019-00041-w&rft_dat=%3Cproquest_cross%3E2354150731%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c347t-ff575f415d219b67c8abecd45831b9365aa77c715deedc2d6495e759789f578e3%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=2354150731&rft_id=info:pmid/32048266&rfr_iscdi=true |