Synthesis of O2- and N3-(2-Phosphonomethoxy)ethyl Derivatives of 6-Phenyl- and 6-Pyridinyl-5-azacytosine
摘要:
A series of hydrolytically stable O-2- and N-3-(2-phosphonomethoxy)ethyl (PME) derivatives of 6-phenyl, pyridin-2, -3 and -4-yl-5-azacytosines was prepared by their alkylation with diisopropyl (2-chloroethoxy)methylphosphonate followed by the deprotection. No antitumor or antiviral activity was found except for 6-(pyridin-4-yl)-1,3,5-triazine-2,4-diamine (13d) which exhibited slight activity against feline herpesvirus in CrFK cell cultures with IC50 = 6.7 mu g/mL.
Synthesis of O2- and N3-(2-Phosphonomethoxy)ethyl Derivatives of 6-Phenyl- and 6-Pyridinyl-5-azacytosine
摘要:
A series of hydrolytically stable O-2- and N-3-(2-phosphonomethoxy)ethyl (PME) derivatives of 6-phenyl, pyridin-2, -3 and -4-yl-5-azacytosines was prepared by their alkylation with diisopropyl (2-chloroethoxy)methylphosphonate followed by the deprotection. No antitumor or antiviral activity was found except for 6-(pyridin-4-yl)-1,3,5-triazine-2,4-diamine (13d) which exhibited slight activity against feline herpesvirus in CrFK cell cultures with IC50 = 6.7 mu g/mL.
The present invention relates to a system comprising a genetic construct a riboswitch operably linked to a regulatory sequence, and a second genetic construct a coding sequence whose expression is capable of being regulated by a gene product of the first construct. Also provided is a genetic construct comprising one or more riboswitches for regulation of gene expression, wherein preferably a spacer sequence is provided downstream of the riboswitch to enhance expression of a coding sequence which is operably linked to a riboswitch. Ligands, kits, methods, host cells and expression systems are also provided.
Synthesis of O2- and N3-(2-Phosphonomethoxy)ethyl Derivatives of 6-Phenyl- and 6-Pyridinyl-5-azacytosine
A series of hydrolytically stable O-2- and N-3-(2-phosphonomethoxy)ethyl (PME) derivatives of 6-phenyl, pyridin-2, -3 and -4-yl-5-azacytosines was prepared by their alkylation with diisopropyl (2-chloroethoxy)methylphosphonate followed by the deprotection. No antitumor or antiviral activity was found except for 6-(pyridin-4-yl)-1,3,5-triazine-2,4-diamine (13d) which exhibited slight activity against feline herpesvirus in CrFK cell cultures with IC50 = 6.7 mu g/mL.