Compounds > 4-5-6-7-tetrabromobenzimidazole

4-5-6-7-tetrabromobenzimidazole and Prostatic-Neoplasms

4-5-6-7-tetrabromobenzimidazole has been researched along with Prostatic-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for 4-5-6-7-tetrabromobenzimidazole and Prostatic-Neoplasms

Article	Year
Modified tetrahalogenated benzimidazoles with CK2 inhibitory activity are active against human prostate cancer cells LNCaP in vitro. Bioorganic & medicinal chemistry, 2012, Jul-15, Volume: 20, Issue:14 A series of novel CK2 inhibitors, tetrahalogenated benzimidazoles carrying an aminoalkylamino group at position 2, has been prepared by nucleophilic substitution of the respective 2,4,5,6,7-pentabromobenzimidazoles and 2-bromo-4,5,6,7-tetraiodobenzimidazoles. The new derivatives as well as some previously obtained tetrahalogenobenzimidazoles, including 4,5,6,7-tetrabromobenzimidazole (TBI) and 4,5,6,7-tetraiodobenzimidazole (TIBI), were evaluated for activity against the hormone-sensitive human prostate cancer cell line LNCaP. The activity of 2-aminoalkylamino derivatives was notably higher (LD(50) 4.75-9.37 μM) than that of TBI and TIBI (LD(50) ≈ 20 μM). The determination of the LD(50) value identified the 2-aminoethylamino-4,5,6,7-tetraiodobenzimidazole with an additional methyl group at position 1 (6) as the most efficient compound (LD(50): 4.75 ± 1.02 μM). Interestingly, there was no clear correlation between cell viability and apoptosis induction indicating additional cell death mechanisms. Topics: Antineoplastic Agents; Apoptosis; Benzimidazoles; Casein Kinase II; Cell Line, Tumor; Humans; Male; Prostatic Neoplasms; Protein Kinase Inhibitors	2012

Article

Year

Modified tetrahalogenated benzimidazoles with CK2 inhibitory activity are active against human prostate cancer cells LNCaP in vitro.

Bioorganic & medicinal chemistry, 2012, Jul-15, Volume: 20, Issue:14

A series of novel CK2 inhibitors, tetrahalogenated benzimidazoles carrying an aminoalkylamino group at position 2, has been prepared by nucleophilic substitution of the respective 2,4,5,6,7-pentabromobenzimidazoles and 2-bromo-4,5,6,7-tetraiodobenzimidazoles. The new derivatives as well as some previously obtained tetrahalogenobenzimidazoles, including 4,5,6,7-tetrabromobenzimidazole (TBI) and 4,5,6,7-tetraiodobenzimidazole (TIBI), were evaluated for activity against the hormone-sensitive human prostate cancer cell line LNCaP. The activity of 2-aminoalkylamino derivatives was notably higher (LD(50) 4.75-9.37 μM) than that of TBI and TIBI (LD(50) ≈ 20 μM). The determination of the LD(50) value identified the 2-aminoethylamino-4,5,6,7-tetraiodobenzimidazole with an additional methyl group at position 1 (6) as the most efficient compound (LD(50): 4.75 ± 1.02 μM). Interestingly, there was no clear correlation between cell viability and apoptosis induction indicating additional cell death mechanisms.

Topics: Antineoplastic Agents; Apoptosis; Benzimidazoles; Casein Kinase II; Cell Line, Tumor; Humans; Male; Prostatic Neoplasms; Protein Kinase Inhibitors

2012