These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: In vitro cytostatic activity of 1,2,4-triazolo- and 1,2,3,4-tetrazolo pyridazines.
    Author: Hładoń B, Laskowska H, Sloderbach A, Melzer E.
    Journal: Pol J Pharmacol; 1997; 49(6):471-7. PubMed ID: 9566051.
    Abstract:
    Out of a series of fourteen 1,2,4-triazolo(4,3-b)-, and 1,2,3,4-tetrazolo-(1,5-b)pyridazine derivatives, 4 compounds have been found to reveal high cytostatic activity in KB and HeLa human cancer cell lines in vitro with ED50 activity values ranging from 0.25 to 3.0 micrograms/cm3 (0.009-0.158 x 10(-4) mole/l), and according to DR and D, NCI, NIH Bethesda criterion were qualified for further in vivo screening investigation. 6-Chloro-8-(N,N-dimethylaminosulfonylmethyl)-1,2,3,4-tetrazolo+ ++-(1,5-b)- pyridazine exhibited the strongest in vitro cytostatic activity (ED50 = 0.009 x 10(-4) mole/l), comparable with the best standards, and higher in comparison with a standard cytosine arabinoside (ED50 = 0.03-0.04 x 10(-4) mole/l). The presence of chlorine atom at C-6 position in the pyridazine ring determines the cytotoxic activity of tetrazolopyridazines as the primary factor and C-8 substituents, which influence their better solubility seems to be a secondary one, as confirmed by the results of the structure-activity and solubility-activity relationship analysis. However, for the exhibition of the triazolopyridazine activities the presence of two chlorine atoms at C-6 and C-3 position was essential.
    [Abstract] [Full Text] [Related] [New Search]