93065-62-4Relevant articles and documents
PRODRUGS FOR NITROREDUCTASE BASED CANCER THERAPY- 2: Novel amide/Ntr combinations targeting PC3 cancer cells
Güng?r, Tu?ba,?nder, Ferah C?mert,Tokay, Esra,Gülhan, ünzile Güven,Hac?o?lu, Nelin,Tok, Tu?ba Ta?k?n,?elik, Ayhan,K??kar, Feray,Ay, Mehmet
, p. 383 - 400 (2019/04/01)
The use of nitroreductases (NTR) that catalyze the reduction of nitro compounds by using NAD(P)H in GDEPT (Gene-directed enzyme prodrug therapy) studies which minimize toxicity at healthy cells and increases concentration of drugs at cancer cells is remarkable. Discovery of new prodrug/NTR combinations is necessary to be an alternative to known prodrug candidates such as CB1954, SN23862, PR-104A. For this aim, nitro containing aromatic amides (A1-A23) were designed, synthesized, performed in silico ADMET and molecular docking techniques in this study. Prodrug candidates were studied on reduction potentials with Ssap-NtrB by HPLC system. Also, cyototoxic properties and prodrug ability of these amides were investigated using different cancer cell lines such as Hep3B and PC3. As a result of theoretical and biological studies, combinations of A5, A6 and A20 with Ssap-NtrB can be suggested as potential prodrugs/enzyme combinations at NTR based cancer therapy compared with CB1954/NfsB.
Reaction of piperazine with trimethylacetic arylcarboxylic anhydride; a convenient method for preparing monoacylated piperazine derivatives
Lai,Wang,Luh
, p. 361 - 363 (2007/10/03)
A series of monosubstituted piperazine derivatives were obtained by the reaction of piperazine with trimethylacetic arylcarboxylic anhydrides in good yields, which were prepared in situ from arylcarboxylic acid with trimethylacetyl chloride in the presence of triethylamine.