5922-25-8Relevant academic research and scientific papers
Synthesis method of 2-(4-aminophenyl)-5-aminobenzimidazole
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Paragraph 0239-0242; 0244-0245, (2022/01/20)
The present invention provides a synthesis method of 2- (4-aminophenyl)-5-aminobenzimidazole, comprising the following steps: step 1, preparation of N,N'-bis (4-nitro - α- chlorinated) phenylmethylene p-phenylenediamine; step 2, using N, N'-bis(4-nitro - α- chloro) phenylmethylene p-phenylenediamine preparation N, N'-bis (4-nitro - α - imino) benzyl p-phenylenediamine; step 3, using N, N'-di (4-nitro - α - imino) benzyl p-phenylenediamine preparation 2- ( Step 4, 2-(4-nitro)phenyl-5-aminobenzimidazole was hydrogenated with a hydrogenation catalyst and hydrogen to give 2-(4-amino)phenyl-4-aminobenzimidazole. The present invention is intended to achieve a low production cost and high safety, less harmful pollutants 2- (4-aminophenyl) -5-aminobenzimidazole synthesis method.
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.
