Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)- 2H-phthalazin-1-ones as potent PARP-1 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 16, 2014, Pages 3739-3743

  Wang, Ling Xiao ^a   Zhou, Xin Bo ^a   Xiao, Meng Liang ^a   Jiang, Ning ^a   Liu, Feng ^a   Zhou, Wen Xia ^a   Wang, Xiao Kui ^a   Zheng, Zhi Bing ^a   Li, Song ^a  

^a BEIJING INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY   (China)

Author keywords

4 (Thiophen 2 ylmethyl) 2H phthalazin 1 ones; Antitumor; Biological evaluation; PARP 1 inhibitor; Synthesis

Indexed keywords

GLYCOSYLTRANSFERASE INHIBITOR; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE 1; OLAPARIB; PHTHALAZINE DERIVATIVE; ENZYME INHIBITOR; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; PARP1 PROTEIN, HUMAN; THIOPHENE DERIVATIVE;

ARTICLE; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HYDROGEN BOND; IC50; NUCLEOPHILICITY; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; METABOLISM; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; HUMANS; MOLECULAR STRUCTURE; PHTHALAZINES; POLY(ADP-RIBOSE) POLYMERASES; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES;

EID: 84905924721     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.07.001     Document Type: Article

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