Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors
The synthesis and biological evaluation of a new series of amine-substituted 2-arylbenzimidazole-4-carboxamide inhibitors of the DNA-repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) is reported. The introduction of an amine substituent at the 2-aryl position is not detrimental to activity, with most inhibitors exhibiting K(i) values for PARP-1 inhibition in the low nanomolar range. Two compounds in this series were found to potentiate the cytotoxicity of the DNA-methylating agent temozolomide by 4-5-fold in a human colorectal cancer cell line.
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
2004 |
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| Erschienen: |
2004 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:14 |
|---|---|
| Enthalten in: |
Bioorganic & medicinal chemistry letters - 14(2004), 10 vom: 17. Mai, Seite 2433-7 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
White, Alex W [VerfasserIn] |
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| Themen: |
7GR28W0FJI |
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| Anmerkungen: |
Date Completed 22.12.2004 Date Revised 30.11.2018 published: Print Citation Status MEDLINE |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM148015476 |
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| 100 | 1 | |a White, Alex W |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors |
| 264 | 1 | |c 2004 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ohne Hilfsmittel zu benutzen |b n |2 rdamedia | ||
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| 500 | |a Date Completed 22.12.2004 | ||
| 500 | |a Date Revised 30.11.2018 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a The synthesis and biological evaluation of a new series of amine-substituted 2-arylbenzimidazole-4-carboxamide inhibitors of the DNA-repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) is reported. The introduction of an amine substituent at the 2-aryl position is not detrimental to activity, with most inhibitors exhibiting K(i) values for PARP-1 inhibition in the low nanomolar range. Two compounds in this series were found to potentiate the cytotoxicity of the DNA-methylating agent temozolomide by 4-5-fold in a human colorectal cancer cell line | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 7 | |a Amides |2 NLM | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Benzimidazoles |2 NLM | |
| 650 | 7 | |a Poly(ADP-ribose) Polymerase Inhibitors |2 NLM | |
| 650 | 7 | |a Dacarbazine |2 NLM | |
| 650 | 7 | |a 7GR28W0FJI |2 NLM | |
| 650 | 7 | |a Temozolomide |2 NLM | |
| 650 | 7 | |a YF1K15M17Y |2 NLM | |
| 700 | 1 | |a Curtin, Nicola J |e verfasserin |4 aut | |
| 700 | 1 | |a Eastman, Brian W |e verfasserin |4 aut | |
| 700 | 1 | |a Golding, Bernard T |e verfasserin |4 aut | |
| 700 | 1 | |a Hostomsky, Zdenek |e verfasserin |4 aut | |
| 700 | 1 | |a Kyle, Suzanne |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Jianke |e verfasserin |4 aut | |
| 700 | 1 | |a Maegley, Karen A |e verfasserin |4 aut | |
| 700 | 1 | |a Skalitzky, Donald J |e verfasserin |4 aut | |
| 700 | 1 | |a Webber, Stephen E |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Xiao-Hong |e verfasserin |4 aut | |
| 700 | 1 | |a Griffin, Roger J |e verfasserin |4 aut | |
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