22794-92-9Relevant academic research and scientific papers
Synthesis, In Vitro α-Amylase Activity, and Molecular Docking Study of New Benzimidazole Derivatives
Aziz, A.,Khan, F.,Mubeen, S.,Rahim, F.,Sarfraz, M.,Shah, S. A. Ali,Taha, M.,Uddin, I.,Ullah, Hafeez,Ullah, Hayat
, p. 968 - 975 (2021/07/22)
Abstract: New benzimidazole derivatives were synthesized by reacting substitutedphenacyl bromides with 1H-benzimidazole-2-thiols. The synthesized compounds werecharacterized through 1H and13C NMR and high-resolution mass spectra. The
Synthesis of benzimidazole derivatives as potent inhibitors for α-amylase and their molecular docking study in management of type-II diabetes
Hussain, Shafqat,Taha, Muhammad,Rahim, Fazal,Hayat, Shawkat,Zaman, Khalid,Iqbal, Naveed,Selvaraj, Manikandan,Sajid, Muhammad,Bangesh, Masroor Ahmad,Khan, Fahad,Khan, Khalid Mohammed,Uddin, Nizam,Shah, Syed Adnan Ali,Ali, Muhammad
, (2021/02/21)
In the search of potent α-amylase inhibitors, we have synthesized seventeen derivatives of 2-mercaptobenzimidazole bearing sulfonamide (1–17) and evaluated for their α-amylase inhibitory potential. All synthesized compounds display a variable degree of α-amylase activity having IC50 values ranging between 0.90 ± 0.05 to 11.20 ± 0.30 μM when compared with the standard drug acarbose having IC50 value 1.70 ± 0.10 μM. Compound 1, 2, 11, 12 and 14 having IC50 values 1.40 ± 0.10, 1.30 ± 0.05, 0.90 ± 0.05, 1.60 ± 0.05 and 1.60 ± 0.10 μM respectively were found many folds better than the standard drug acarbose. While others derivatives of the series showed good inhibitory potentials. All the synthesized compounds were characterized by HREI-MS, 1H and 13C NMR spectroscopy. Structure activity relationship (SAR) has been established for all newly synthesized analogs. Binding interactions between ligands and active residues of the enzyme were confirmed through molecular docking study.
Synthesis, in vitro alpha-glucosidase inhibitory potential of benzimidazole bearing bis-Schiff bases and their molecular docking study
Rahim, Fazal,Zaman, Khalid,Taha, Muhammad,Ullah, Hayat,Ghufran, Mehreen,Wadood, Abdul,Rehman, Wajid,Uddin, Nizam,Shah, Syed Adnan Ali,Sajid, Muhammad,Nawaz, Faisal,Khan, Khalid Mohammed
, (2019/11/16)
Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop
Synthesis, crystal study, and anti-proliferative activity of some 2-benzimidazolylthioacetophenones towards triple-negative breast cancer MDA-MB-468 cells as apoptosis-inducing agents
Abdel-Aziz, Hatem A.,Eldehna, Wagdy M.,Ghabbour, Hazem,Al-Ansary, Ghada H.,Assaf, Areej M.,Al-Dhfyan, Abdullah
, (2016/08/05)
On account of its poor prognosis and deficiency of therapeutic stratifications, triple negative breast cancer continues to form the causative platform of an incommensurate number of breast cancer deaths. Aiming at the development of potent anticancer agents as a continuum of our previous efforts, a novel series of 2-((benzimidazol-2-yl)thio)-1-arylethan-1-ones 5a–w was synthesized and evaluated for its anti-proliferative activity towards triple negative breast cancer (TNBC) MDA-MB-468 cells. Compound 5k was the most active analog against MDA-MB-468 (IC50 = 19.90 ± 1.37 μM), with 2.1-fold increased activity compared to 5-fluorouracil (IC50 = 41.26 ± 3.77 μM). Compound 5k was able to induce apoptosis in MDA-MB-468, as evidenced by the marked boosting in the percentage of florecsein isothiocyanate annexin V (Annexin V–FITC)-positive apoptotic cells (upper right (UR) + lower right (LR)) by 2.8-fold in comparison to control accompanied by significant increase in the proportion of cells at pre-G1 (the first gap phase) by 8.13-fold in the cell-cycle analysis. Moreover, a quantitative structure activity relationship (QSAR) model was established to investigate the structural requirements orchestrating the anti-proliferative activity. Finally, we established a theoretical kinetic study.
2-((Benzimidazol-2-yl)thio)-1-arylethan-1-ones: Synthesis, crystal study and cancer stem cells CD133 targeting potential
Abdel-Aziz, Hatem A.,Ghabbour, Hazem A.,Eldehna, Wagdy M.,Al-Rashood, Sara T.A.,Al-Rashood, Khalid A.,Fun, Hoong-Kun,Al-Tahhan, Mays,Al-Dhfyan, Abdullah
, p. 1 - 10 (2015/10/12)
In order to develop a potent anti-tumor agent that can target both cancer stem cells and the bulk of tumor cells, a series of 2-((benzimidazol-2-yl)thio)-1-arylethan-1-ones 5a-o was synthesized. All compounds were evaluated for their anti-proliferative activity towards colon HT-29 cancer cell line. In addition, their inhibitory effect against cell surface expression of CD133, a potent cancer stem cells (CSCs) marker, in the same cells was evaluated by flow cytometry at 10 μM. Compound 5l emerged as the most active anti-proliferative analog against HT-29 (IC50 Combining double low line 18.83 ± 1.37 μM), that almost equipotent as 5-fluorouracil (IC50 Combining double low line 15.83 ± 1.63 μM) with 50.11 ± 4.05% inhibition effect on CD133 expression, suggested dual targeted effect. Also, compounds 5h, 5j, 5k and 5m-o inhibited the expression of CD133 with more than 50%. The SAR study pointed out the significance of substitution of the pendent phenyl group with lipophilic electron-donating groups or replacing it by 2-thienyl or 2-furyl groups.
