1-β-d-Arabinofuranosylcytosine-5′-alkylphosphonophosphates and diphosphates: new orally active derivatives of ara-C

1-beta-D-Arabinofuranosylcytosine-5'-alkylphosphonophosphates and diphosphates: new orally active derivatives of ara-C.

ara-Cytidine-5'-alkylphosphonophosphates and the corresponding -diphosphates were found to be cytostatically active in vitro against the human mammary epithelial cell line H184 A1N4 and the human mammary tumor cell line MaTu. Our results indicate that the replacement of the diphosphate by the phosphonophosphate group has no influence on antiproliferative activity in this case. The compounds wer...

Close Correlation of 1-β-D-Arabinofuranosylcytosine 5'-Triphosphate, an Intracellular Active Metabolite, to the Therapeutic Efficacy of N4-Behenoyl-1-β-D-arabinofuranosylcytosine Therapy for Acute Myelogenous Leukemia

Synthesis of 1-benzothiepine and 1-benzazepine derivatives as orally active CCR5 antagonists.

Quaternary ammonium benzocycloheptene compound 1 has previously been reported as a clinical candidate for an injectable CCR5 antagonist. In order to develop an orally active CCR5 antagonist, derivatives of tertiary amine benzocycloheptene 2, the chemical precursor to 1, were investigated. The benzocycloheptene ring was converted to benzothiepine and benzazepine rings and it was found that these...

Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.

The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none. Incorporation of a fluorine atom in the beta-position to the amino function in the side chain led to analogues that exhibited, in general, enhanced and long-lasting 5-HT1A agonist a...

Shirakawa Cell Cycle - d - Arabinofuranosylcytosine in the β The Locus of Action of 1 - Updated

son Hospital. The cultures were maintained in McCoy's 5A medium reconstituted from powder (Grand Island Biological Company) not containing antibiotics. The medium was supple mented with 20% fetal calf serum (Hyland). The cultures were fed daily and subcultured at least every two days. son Hospital. The KB cells were maintained in minimal essen tial medium (Eagle's) obtained in powdered form fro...