دورية أكاديمية
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors
العنوان: | Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors |
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المؤلفون: | White, Alex William, Curtin, Nicola J., Eastman, Brian W., Golding, Bernard T., Hostomsky, Zdenek, Kyle, Suzanne, Li, Jianke, Maegley, Karen A., Skalitzky, Donald J., Webber, Stephen E., Yu, Xiao-Hong, Griffin, Roger J. |
بيانات النشر: | Elsevier |
سنة النشر: | 2004 |
المجموعة: | Cardiff University: ORCA (Online Research @ Cardiff) |
مصطلحات موضوعية: | RS Pharmacy and materia medica |
الوصف: | 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 Ki 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. |
نوع الوثيقة: | article in journal/newspaper |
اللغة: | unknown |
العلاقة: | White, Alex William https://orca.cardiff.ac.uk/view/cardiffauthors/A047998H.htmlTest orcid:0000-0002-1539-0158 orcid:0000-0002-1539-0158, Curtin, Nicola J., Eastman, Brian W., Golding, Bernard T., Hostomsky, Zdenek, Kyle, Suzanne, Li, Jianke, Maegley, Karen A., Skalitzky, Donald J., Webber, Stephen E., Yu, Xiao-Hong and Griffin, Roger J. 2004. Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors. Biorganic and Medicinal Chemistry Letters 14 (10) , pp. 2433-2437. 10.1016/j.bmcl.2004.03.017 https://doi.org/10.1016/j.bmcl.2004.03.017Test |
DOI: | 10.1016/j.bmcl.2004.03.017 |
الإتاحة: | https://doi.org/10.1016/j.bmcl.2004.03.017Test https://orca.cardiff.ac.uk/id/eprint/68212Test/ |
رقم الانضمام: | edsbas.EB1F1D16 |
قاعدة البيانات: | BASE |
DOI: | 10.1016/j.bmcl.2004.03.017 |
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