30065-33-9Relevant articles and documents
Synthesis of Some Novel Benzimidazole Derivatives as Anticancer Agent and Evaluation for CDK2 Inhibition Activity
El-Hameed, Rania Helmy Abd,Fatahala, Samar Said,Sayed, Amira Ibrahim
, p. 238 - 248 (2022/02/10)
Background: Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules; they can easily interact with biomolecules of living systems. Objective: A series of substituted 2-thiobezimidazoles have been synthesized. Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell lines. Methods: The spectral data of the synthesized compounds were characterized. A docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib, were performed. Results: Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in the CDK-ATP binding pocket .3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib. Conclusion: Against all tested compounds; two compounds 3c &3l were found active against two types of cell-lines.
Synthesis, biological evaluation and molecular modeling studies of N-aryl-2-arylthioacetamides as non-nucleoside HIV-1 reverse transcriptase inhibitors
Xiaohe, Zhu,Yu, Qin,Hong, Yan,Xiuqing, Song,Rugang, Zhong
, p. 330 - 339 (2011/12/22)
A series of N-aryl-2-arylthioacetamide derivatives (2-4) designed as non-nucleoside reverse transcriptase inhibitors was synthesized and evaluated for their inhibitory activity against HIV-1 (IIIB) replication in MT-4 cell cultures. The compounds 2-4 were