Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer
<p>Abstract</p> <p>A new chemical series of antiproliferative compounds was identified <it>via </it>high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 μM). Exploration of the two peripheral diversity vectors of the hit mol...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
BMC
2010-03-01
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| Series: | Chemistry Central Journal |
| Online Access: | http://journal.chemistrycentral.com/content/4/1/4 |
| _version_ | 1818387810270314496 |
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| author | Soldatkina Olga Godovykh Elena Karapetian Ruben Sosnov Andrey V Rufanov Konstantin A Krasavin Mikhail Lavrovsky Yan Gakh Andrei A |
| author_facet | Soldatkina Olga Godovykh Elena Karapetian Ruben Sosnov Andrey V Rufanov Konstantin A Krasavin Mikhail Lavrovsky Yan Gakh Andrei A |
| author_sort | Soldatkina Olga |
| collection | DOAJ |
| description | <p>Abstract</p> <p>A new chemical series of antiproliferative compounds was identified <it>via </it>high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 μM). Exploration of the two peripheral diversity vectors of the hit molecule in a hit-targeted library and testing of the resulting compounds led to SAR generalizations and identification of the 'best' pharmacophoric moieties. The latter were merged in a single compound that exhibited a 200-fold better potency than the original hit compound. Specific cancer cell cytotoxicity was confirmed for the most potent compounds.</p> |
| first_indexed | 2024-12-14T04:15:51Z |
| format | Article |
| id | doaj.art-d68b1386bf9149b2a80920b778b18691 |
| institution | Directory Open Access Journal |
| issn | 1752-153X |
| language | English |
| last_indexed | 2024-12-14T04:15:51Z |
| publishDate | 2010-03-01 |
| publisher | BMC |
| record_format | Article |
| series | Chemistry Central Journal |
| spelling | doaj.art-d68b1386bf9149b2a80920b778b186912022-12-21T23:17:33ZengBMCChemistry Central Journal1752-153X2010-03-0141410.1186/1752-153X-4-4Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancerSoldatkina OlgaGodovykh ElenaKarapetian RubenSosnov Andrey VRufanov Konstantin AKrasavin MikhailLavrovsky YanGakh Andrei A<p>Abstract</p> <p>A new chemical series of antiproliferative compounds was identified <it>via </it>high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 μM). Exploration of the two peripheral diversity vectors of the hit molecule in a hit-targeted library and testing of the resulting compounds led to SAR generalizations and identification of the 'best' pharmacophoric moieties. The latter were merged in a single compound that exhibited a 200-fold better potency than the original hit compound. Specific cancer cell cytotoxicity was confirmed for the most potent compounds.</p>http://journal.chemistrycentral.com/content/4/1/4 |
| spellingShingle | Soldatkina Olga Godovykh Elena Karapetian Ruben Sosnov Andrey V Rufanov Konstantin A Krasavin Mikhail Lavrovsky Yan Gakh Andrei A Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer Chemistry Central Journal |
| title | Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer |
| title_full | Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer |
| title_fullStr | Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer |
| title_full_unstemmed | Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer |
| title_short | Discovery and SAR exploration of <it>N</it>-aryl-<it>N</it>-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer |
| title_sort | discovery and sar exploration of it n it aryl it n it 3 aryl 1 2 4 oxadiazol 5 yl amines as potential therapeutic agents for prostate cancer |
| url | http://journal.chemistrycentral.com/content/4/1/4 |
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