Published 1995 | Version v1
Journal article

In vitro anti-leukemic activity and chemical transformation of the 5'-chloro-5'-deoxy derivative of cyclo-cytidine

  • 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, 83232 Bratislava (Slovak Republic)
  • 2. Department of Experimental Therapy, Cancer Research Institute, Slovak Academy of Sciences, Bratislava (Slovak Republic)
  • 3. Institute of Chemical Drugs, Faculty of Pharmacy, The University of Veterinary Medicine and Pharmacy, Brno (Czech Republic)

Description

Hydrochloride of 5'-chloro-5'-deoxy-cytocytidine (Cl-cC) is an analogue of hydrochloride (cC), a pro-drug of the compound with of the compound with the strong anti-leukemic activity arabinosylcytosine (araC). This paper is devoted to the study of its cytotoxic activity in vitro and to the effect of acid alkaline conditions and temperature on its stability. Cl-cC inhibits not only the growth of L1210 leukemia cells in vitro and the DNA synthesis (IC50 = 0.09 μmol/dm3) but, at the same time, it has a weak effect on RNA synthesis (IC50 > 250 μmol/dm3) and no effect on proteosynthesis. In alkaline conditions Cl-cC is transformed to 5'-chloro-araC and 2',5'-anhydro-araC but is more stable in acid solutions. (author)

Additional details

Publishing Information

Journal Title
Neoplasma
Journal Volume
42
Journal Issue
5
Journal Page Range
p. 255-258
ISSN
0028-2685

Optional Information

Contract/Grant/Project number
Grant SAS-1331
Notes
1 fig., 2 tabs., 17 refs.