The mechanism of the depletion of ATP, recorded in the erythrocytes of adenosine deaminase-deficient children and of leukemia patients treated with deoxycoformycin, »asinvestigated in normal human eryth rocytes treated with this inhibitor of adenosine deaminase. Deoxyadeno sine, which accumulates in both clinical conditions, provoked a dosedependent accumulation of dATP, depletion of ATP, and ...

PURPOSE Chronic lymphocytic leukemia (CLL) lymphocytes respond to DNA alkylation by excision repair, with the extent of repair increasing as the cells acquire resistance to alkylating agents. Because incorporation of nucleotide analogues into the repair patches elicits death signals in quiescent cells, the increased capacity for excision repair in alkylator-resistant cells could facilitate inco...

The analogous imino-variant of the Nazarov reaction suffers from unfavorable energetics associated with the ring closure process, thereby limiting the utility of this class of reactions. In this report, the realization of the first intermolecular interrupted imino-Nazarov reaction utilizing silylated pyrimidine derivatives as nucleophilic trapping partners culminated in an expedient synthetic r...

This review presents a brief account of the chemistry and mechanistic aspects of aryl H-phosphonates, and selected applications of this class of compounds as intermediates in the synthesis of a wide range of biologically important analogues of nucleoside phosphates, and oligonucleotides, in which the phosphate moieties are replaced by other structurally related groups. The aryl nucleoside H-pho...

Rene Csuk, Anja Kern, and Kristina Mohr Institut für Organische Chemie. Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany Reprint requests to Prof. Dr. R. Csuk. E-mail: [email protected] Z. Naturforsch. 54b, 1463-1468 (1999); received July 9, 1999 Nucleoside Analogues, HPLC A novel class of nucleoside analogues containing adenine, uracil, thym...

Hairy-cell leukemia (HCL) is a rare hematologic malignancy. HCL diagnosis can be difficult and the variant form of HCL (HCL-V) has similarities with B-cell prolymphocytic leukemia or splenic marginal zone lymphoma. We describe the different features of HCL, particularly typical HCL (HCL-C) and HCL-V. HCL prognosis was transformed by the introduction of purine nucleoside analogues such as Cladri...

(Carbo)nucleoside derivatives constitute an important class of pharmaceuticals, yet there are only few convergent methods to access new analogues. Here, we report the first synthesis of thymine-, uracil-, and 5-fluorouracil-substituted diester donor-acceptor cyclopropanes and their use in the indium- and tin-catalyzed [3+2] annulations with aldehydes, ketones, and enol ethers. The obtained dies...

Despite the increased understanding of colorectal cancer and the introduction of targeted drug therapy, the metastatic phase of the disease remains refractory to treatment. Since the deregulation of normal apoptosis contributes to the pathogenesis of colorectal cancer, novel nucleoside analogues were synthesized here and evaluated for their ability to induce apoptosis and cause cell death in tw...