- Synthetic studies towards the development of psoralen-acidic retinoid conjugates and hybrids
-
The chemical modification of trioxsalen using electrophilic aromatic substitution reactions, followed by either Wittig or Heck reactions or Suzuki coupling, allowed for ready access to C4′ modified trioxsalen derivatives that were successfully used for th
- Militsopoulou, Maria,Bariamis, Stavros E.,Athanassopoulos, Constantinos M.,Papaioannou, Dionissios
-
experimental part
p. 3433 - 3442
(2009/05/26)
-
- Compositions and methods for targeted enzymatic release of cell regulatory compounds
-
Novel pro-drugs and methods for their use to alter the growth and biological characteristics of living cells, tissues, or whole organisms are described. The methods allow for selective activation of the pro-drugs at or near transformant host cells expressing a gene for an enzyme that activates the pro-drugs. Pro-drugs according to a preferred embodiment of the invention are conjugates of a bioactive compound and a chemical group that is capable of being cleaved from the bioactive compound by action of an enzyme. Methods according to this invention include, (a) introducing into targeted cells a gene encoding an enzyme and (b) administering a pro-drug, wherein the enzyme releases the pro-drug from conjugation. In a preferred embodiment of the invention, the gene encoding the enzyme is a marker gene.
- -
-
Page column 15
(2010/02/05)
-
- Psoralens
-
New psoralen compounds have been synthesized. The compounds all include the addition of substituent groups at the 4' position on the basic trioxsalen structure. Specifically, the compounds have the structure: STR1 wherein X may be any desired substituent such as halogenated alkyls, alcohols, ethers, aminoalkyls, etc. The new substituted psoralens exhibit high solubility in aqueous solution and low dissociation constants from deoxyribonucleic acid (DNA), as well as a reactivity with ribonucleic acids (RNA). Such psoralen compounds find use in the study of secondary structures of nucleic acids; as inhibitors of RNA replication; in the inactivation of viruses; and in the photo chemotherapy of psoriasis.
- -
-
-