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Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 20, 2013, Pages 5660-5666

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase

(9) Rosenthal, Andrew S a Dexheimer, Thomas S a Gileadi, Opher b Nguyen, Giang H c,d Chu, Wai Kit e Hickson, Ian D c,e Jadhav, Ajit a Simeonov, Anton a Maloney, David J a

a NATIONAL INSTITUTES OF HEALTH (United States)

b UNIVERSITY OF OXFORD (United Kingdom)

c UNIVERSITY OF OXFORD (United Kingdom)

d NATIONAL CANCER INSTITUTE (United States)

e UNIVERSITY OF COPENHAGEN (Denmark)

Author keywords

Bloom helicase; Inhibitor; Small molecule

Indexed keywords

1,3,4 THIADIAZOLE DERIVATIVE; 5 (PYRIDIN 4 YL) 1,3,4 THIADIAZOL 2 AMINE; ADENOSINE TRIPHOSPHATASE; ANTINEOPLASTIC AGENT; BLOOM SYNDROME HELICASE; DOUBLE STRANDED DNA; ENZYME INHIBITOR; ML 216; MLS 000559245; NSC 19630; RECQ HELICASE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; BLOOM SYNDROME; CANCER SUSCEPTIBILITY; DNA DENATURATION; DNA REPAIR; DNA STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; GENE PRODUCT; HIGH THROUGHPUT SCREENING; HOLLIDAY JUNCTION; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; PHYSICAL CHEMISTRY; SISTER CHROMATID EXCHANGE; STRUCTURE ACTIVITY RELATION;

[1,3-BIS(2,6-DIISOPROPYLPHENYL)IMIDAZOLE-2-YLIDENE](3-CHLOROPYRIDYL)PALLADIUM(II)CHLORIDE; ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION; ADME; BLM; BLOOM HELICASE; BLOOM SYNDROME; BS; DIMETHYLFORMAMIDE; DMF; HIGH THROUGHPUT SCREEN; HOMOLOGOUS RECOMBINATION; HR; HTS; INHIBITOR; MLM; MOUSE LIVER MICROSOMES; NADPH; NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE; PBS; PEPPSITM-IPR; PHOSPHATE BUFFERED SALINE; SAR; SCE; SISTER CHROMATID EXCHANGES; SMALL MOLECULE; STRUCTURE ACTIVITY RELATIONSHIP;

AMINES; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; ENZYME INHIBITORS; HUMANS; PHENYLUREA COMPOUNDS; RECQ HELICASES; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES;

EID: 84884279311 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2013.08.025 Document Type: Article

Times cited : (28)

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