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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Veröffentlicht in:	Clinical cancer research 2003-07, Vol.9 (7), p.2711-2718
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	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