Identification of potent nontoxic poly(ADP-ribose) polymerase-1 inhibitors: Chemopotentiation and pharmacological studies

The nuclear enzyme poly(ADP-ribose) polymerase (PARP-1) facilitates DNA repair, and is, therefore, an attractive target for anticancer chemo- and radio-potentiation. Novel benzimidazole-4-carboxamides (BZ1-6) and tricyclic lactam indoles (TI1-5) with PARP-1 K(i) values of

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Bibliographic Details
Published in:Clinical cancer research 2003-07, Vol.9 (7), p.2711-2718
Main Authors: CALABRESE, Christopher R, BATEY, Michael A, MAEGLEY, Karen, CALVERT, Alan H, HOSTOMSKY, Zdenek, NEWELL, David R, CURTIN, Nicola J, THOMAS, Huw D, DURKACZ, Barbara W, WANG, Lan-Zhen, KYLE, Suzanne, SKALITZKY, Donald, LI, Janke, ZHANG, Catherine, BORITZKI, Theodore
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - pharmacology
Antineoplastic Agents, Alkylating - pharmacology
Biological and medical sciences
Cell Division
Cell Line, Tumor
Chemotherapy
Dacarbazine - analogs & derivatives
Dacarbazine - therapeutic use
Dacarbazine - toxicity
DNA Repair
Dose-Response Relationship, Drug
Enzyme Inhibitors - pharmacology
Humans
Indoles - metabolism
Kinetics
Medical sciences
Models, Chemical
Pharmacology. Drug treatments
Poly(ADP-ribose) Polymerase Inhibitors
Poly(ADP-ribose) Polymerases - genetics
Temperature
Time Factors
Tissue Distribution
Topotecan - therapeutic use
Topotecan - toxicity
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Description
Summary:The nuclear enzyme poly(ADP-ribose) polymerase (PARP-1) facilitates DNA repair, and is, therefore, an attractive target for anticancer chemo- and radio-potentiation. Novel benzimidazole-4-carboxamides (BZ1-6) and tricyclic lactam indoles (TI1-5) with PARP-1 K(i) values of
ISSN:1078-0432
1557-3265