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

Rosenthal, Andrew S; Dexheimer, Thomas S; Gileadi, Opher; Nguyen, Giang H; Chu, Wai Kit; Hickson, Ian D; Jadhav, Ajit; Simeonov, Anton; Maloney, David J

Rosenthal, Andrew S; Dexheimer, Thomas S; Gileadi, Opher; Nguyen, Giang H; Chu, Wai Kit; Hickson, Ian D; Jadhav, Ajit; Simeonov, Anton; Maloney, David J.

Afiliação

Rosenthal AS; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD, 20892.
Dexheimer TS; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD, 20892.
Gileadi O; The Structural Genomics Consortium, University of Oxford, Oxford OX3 7DQ, UK.
Nguyen GH; Department of Medical Oncology, Weatherall Institute of Molecular Medicine, John Radcliffe Hospital, University of Oxford, Oxford OX3 9DS, UK.
Chu WK; Laboratory of Human Carcinogenesis, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD.
Hickson ID; Department of Cellular and Molecular Medicine, Nordea Center for Healthy Aging, University of Copenhagen, '2200 Copenhagen N, Denmark.
Jadhav A; Department of Medical Oncology, Weatherall Institute of Molecular Medicine, John Radcliffe Hospital, University of Oxford, Oxford OX3 9DS, UK.
Simeonov A; Department of Cellular and Molecular Medicine, Nordea Center for Healthy Aging, University of Copenhagen, '2200 Copenhagen N, Denmark.
Maloney DJ; National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD, 20892.

Bioorg Med Chem Lett ; 23(20): 5660-6, 2013 Oct 15.

Article em En | MEDLINE | ID: mdl-24012121

Assuntos

Aminas/química; Inibidores Enzimáticos/síntese química; Compostos de Fenilureia/síntese química; RecQ Helicases/antagonistas & inibidores; Tiadiazóis/química; Aminas/síntese química; Aminas/farmacologia; Células CACO-2; Permeabilidade da Membrana Celular/efeitos dos fármacos; Inibidores Enzimáticos/química; Inibidores Enzimáticos/farmacologia; Humanos; Compostos de Fenilureia/química; Compostos de Fenilureia/farmacologia; RecQ Helicases/metabolismo; Relação Estrutura-Atividade; Tiadiazóis/síntese química; Tiadiazóis/farmacologia

Palavras-chave

ADME; BLM; BS; Bloom helicase; Bloom syndrome; DMF; HR; HTS; Inhibitor; MLM; NADPH; PBS; PEPPSITM-IPr; SAR; SCE; Small molecule; [1,3-Bis(2,6-Diisopropylphenyl)imidazole-2-ylidene](3-chloropyridyl)palladium(II)chloride; absorption, distribution, metabolism and excretion; dimethylformamide; high throughput screen; homologous recombination; mouse liver microsomes; nicotinamide adenine dinucleotide phosphate; phosphate buffered saline; sister chromatid exchanges; structure activity relationship

Texto completo

Imprimir

XML

PubMed Links

Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Fenilureia / Tiadiazóis / Inibidores Enzimáticos / RecQ Helicases / Aminas Limite: Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article

Texto completo

Imprimir

XML

PubMed Links

Buscar no Google