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In several types of cancers, the expression of carbonic anhydrase-IX (CA-IX) enzyme is elevated than its normal level which ultimately plays a key role in the tumor growth of epithelial cells in breast and lung cancer by acidifying tumor microenvironment, therefore, inhibition of this target is important in antitumor therapy. We have synthesized bis -benzimidazole derivatives (1–25) by using 3,3′-diaminobenzidine and various aromatic aldehydes and characterized by various spectroscopic methods (UV/Visible, 1HNMR, 13CNMR, and mass spectrometry). Their inhibitory potential for human CA-IX (h CA-IX) was evaluated in-vitro , where several synthesized derivatives showed potent inhibition of h CA-IX (IC 50 values in range of 5.23 ± 1.05 to 40.10 ± 1.78 μM) and compounds 3–5 , 7–8 , 13–16 , 21 and 23 showed superior activity than the standard drug "acetazolamide" (IC 50 = 18.24 ± 1.43 μM). Furthermore, all these compounds showed no toxicity on human fibroblast cell lines (BJ cell lines). Moreover, molecular docking was carried out to predict their binding modes in the active site of CA-IX and revealed a significant role of imidazole ring of synthesized entities in their effective binding with the specific residues of CA-IX. The obtained results paved the way for further in vivo and other pharmacological studies for the optimization of these molecules as possible anti-cancer agents. [ABSTRACT FROM AUTHOR]

In several types of cancers, the expression of carbonic anhydrase-IX (CA-IX) enzyme is elevated than its normal level which ultimately plays a key role in the tumor growth of epithelial cells in breast and lung cancer by acidifying tumor microenvironment, therefore, inhibition of this target is important in antitumor therapy. We have synthesized bis -benzimidazole derivatives (1–25) by using 3,3′-diaminobenzidine and various aromatic aldehydes and characterized by various spectroscopic methods (UV/Visible, 1HNMR, 13CNMR, and mass spectrometry). Their inhibitory potential for human CA-IX (h CA-IX) was evaluated in-vitro , where several synthesized derivatives showed potent inhibition of h CA-IX (IC 50 values in range of 5.23 ± 1.05 to 40.10 ± 1.78 μM) and compounds 3–5 , 7–8 , 13–16 , 21 and 23 showed superior activity than the standard drug "acetazolamide" (IC 50 = 18.24 ± 1.43 μM). Furthermore, all these compounds showed no toxicity on human fibroblast cell lines (BJ cell lines). Moreover, molecular docking was carried out to predict their binding modes in the active site of CA-IX and revealed a significant role of imidazole ring of synthesized entities in their effective binding with the specific residues of CA-IX. The obtained results paved the way for further in vivo and other pharmacological studies for the optimization of these molecules as possible anti-cancer agents. [ABSTRACT FROM AUTHOR]

Different films comprising pure chitosan (CS) and chitosan coated sodium zeolites composites films designated as CSZ1, CSZ2, CSZ3 and CSZ4 respectively are presented here for the sequestration of MO dye. The as-synthesized films were characterized by using FSESM, XPS XRD, and TGA analysis. The sequestration of methyl orange dye (MO) was studied under various adsorption parameters i.e. pH effect, reaction temperature, catalytic dosage, interaction period, and original dye concentration in batch experiments. The adsorption power of MO dye sequestration in the presence of CSZ3 was 287 mg g−1 higher than the fine CS (201 mg g−1), and lowest for CSZ4 (173 mg g−1). The experimental data is fitted in the pseudo-second order of chemical kinetics. The Freundlich and Langmuir adsorption models were used on behalf of the analysis of experimental data that revealed multilayered adsorption of MO dye. Kinetics, equilibrium and thermodynamic process were discussed in detailed, suggesting the endothermic and spontaneous process of the adsorption of MO dye on the exterior of films. The present work is general for the MO adsorption, however, it can be applied on large scale applications and can be easily adjustable in the water purification assemblies. Unlabelled Image • Synthesis of CS coated sodium zeolite films • Loading of different weight of sodium zeolite to CS film • Application in the adsorption of MO dye • Kinetics and thermodynamics studies [ABSTRACT FROM AUTHOR]