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| Titel: |
New 1,2,4-triazine bearing compounds: molecular modeling, synthesis and biotesting |
| Auteur: |
Palchykovska L. G. Alexeeva I. V. Platonov M. O. Kostenko O. M. Usenko L. S. Negrutska V. V. Shved A. D. |
| Verschenen in: |
Biopolymers and cell |
| Paginering: | Jaargang 25 (2009) nr. 6 pagina's 491-499 |
| Jaar: |
2009 |
| Inhoud: |
Aim. To enlarge a spectrum of biologically active compounds in the series of the 1,2,4-triazino[5,6-b] [1,4]benzothiazine (1,2,4-TBT) derivatives and reveal among them efficient inhibitors of RNA synthesis Methods. The methods of structure optimization of the 3-oxo-1,2,4-TBT by fragment-oriented substitution, the molecular doking of new structures in a virtual target, the rational chemical synthesis of the theoretically predicted compounds and their testing in the system of transcription in vitro. Results. The series of 1,2,4-TBT derivatives with substituents in the benzene and triazine cycles of a base molecule were synthesized. The testing of synthesized compounds in the in vitro transcription system directed by T7 RNA polymerase revealed the structure- and concentration-dependent inhibition of the RNA synthesis by some of these compounds. The experimental and virtual screening data for all investigated compounds have a good correlation. It was found that most effective derivative is the 3-oxo-8-butyl-1,2,4-TBT which completely inhibited transcription at the concentration of 6 mg/ml. Conclusions. The biotesting results allow us to assume that the inhibition of RNA synthesis is caused by binding of the 3-oxo- 8-butyl-1,2,4-TBT to both free RNA polymerase molecules and those including in a transcriptional complex with DNA |
| Uitgever: |
Institute of molecular biology and genetics, National Academy of Sciences of Ukraine (provided by DOAJ) |
| Bronbestand: |
Elektronische Wetenschappelijke Tijdschriften |
Details van artikel 9 van 11 gevonden artikelen
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