scholarly journals Synthesis, characterization and biological evaluation studies of Cu(II) and Zn(II) complexes with gly-o-andn or gly-p-andn as primary ligand and N, N' donors as secondary ligand

2020 ◽  
Vol 1531 ◽  
pp. 012111
Author(s):  
Nidhi Aggarwal ◽  
Rishi Kant ◽  
Dr. Gaurav Kumar ◽  
Charisma James ◽  
Dr. Suman Maji
2013 ◽  
Vol 22 (12) ◽  
pp. 5823-5831 ◽  
Author(s):  
Mohamed F. Zayed ◽  
Hany E. A. Ahmed ◽  
Abdel-Sattar M. Omar ◽  
Adel S. Abdelrahim ◽  
Khaled El-Adl

2022 ◽  
Author(s):  
Anjila Kumari ◽  
Tara Jaiswal ◽  
Vinay Kumar ◽  
Neha Hura ◽  
Gulshan Kumar ◽  
...  

2-Arylquinazolines with a range of alkyl polyamines as side chain/ring functional motifs at 4th-position were considered for antileishmanial study with the rationale that related heterocyclic scaffolds and the polyamine functionalities...


2021 ◽  
Author(s):  
ulviye acar çevik ◽  
Ismail Celik ◽  
Ayşen IŞIK ◽  
Yusuf Özkay ◽  
Zafer Asım Kaplancıklı

Abstract In this study, due to the potential anticancer effects of the benzimidazole ring system, a series of benzimidazole-1,3,4-oxadiazole derivatives were synthesized and characterized by 1H NMR, 13C NMR, and MS spectra analyses. In the in vitro anticancer assay, all the compounds tested anticancer activities using MTT-based assay against five cancer cell lines (MCF-7, A549, HeLa, C6, and HepG2). Among them, compound 5a exhibited the most potent activity with IC50 values of 5,165±0,211 μM and 5,995±0,264 μM against MCF-7 and HepG2 cell lines. Compound 5a was included in the BrdU test to determine the DNA synthesis inhibition effects for both cell types. Furthermore, compound 5c was also found to be more effective than doxorubicin on the HeLa cell line. The selectivity of anticancer activity was evaluated in NIH3T3 (mouse embryo fibroblast cell line) cell line. In vitro, enzymatic inhibition assays of aromatase enzyme were performed for compound 5a acting on the MCF-7 cell line. For compound 5a, in silico molecular docking against aromatase enzyme was performed to determine possible protein-ligand interactions and binding modes.


2021 ◽  
Vol 37 (2) ◽  
pp. 508-512
Author(s):  
Jaganmohana Rao Saketi ◽  
S N Murthy Boddapati ◽  
Raghuram M ◽  
Geetha Bhavani Koduru ◽  
Haribabu Bollikolla

The in vitroantimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to goodin vitroantimicrobial activities.


2021 ◽  
Author(s):  
Parleen Kaur ◽  
Sonia Sharma ◽  
Vinay Randhawa ◽  
Navneet Agnihotri ◽  
Ramandeep Kaur ◽  
...  

Abstract In the present work, synthesis of 4,5-dehydrospiulosine and its chain analogues (1-3) as potential Sphingosine Kinase I inhibitors has been achieved via the diasteroselective Grignard reaction, stereoselective cross metathesis reaction followed by N-acylation with p-nitrophenyl butyrate to give the corresponding butyrate ceramides (4-6). All compounds were obtained in high yield and purity followed by molecular docking simulation studies using AutoDock which indicated their varying binding affinities with Sphingosine Kinase 1 protein was done. Further, the biological evaluation studies, as potential anti-prostate cancer agents by inhibiting the sphingosine kinase 1 protien of all synthesized compounds (1-6) on PC-3 cell lines by SRB method was done. Compound N-((2S,3S,E)-3 hydroxyheptadec-4-en-2-yl) butyramide (4) exhibited remarkable cytotoxicity with an IC50 value of 6.06 µM.


Materials ◽  
2018 ◽  
Vol 11 (10) ◽  
pp. 1832 ◽  
Author(s):  
Chen-Guang Liu ◽  
Yu-Ting Zeng ◽  
Ranjith Kankala ◽  
Shan-Shan Zhang ◽  
Ai-Zheng Chen ◽  
...  

Some basic requirements of bone tissue engineering include cells derived from bone tissues, three-dimensional (3D) scaffold materials, and osteogenic factors. In this framework, the critical architecture of the scaffolds plays a crucial role to support and assist the adhesion of the cells, and the subsequent tissue repairs. However, numerous traditional methods suffer from certain drawbacks, such as multi-step preparation, poor reproducibility, high complexity, difficulty in controlling the porous architectures, the shape of the scaffolds, and the existence of solvent residue, which limits their applicability. In this work, we fabricated innovative poly(lactic-co-glycolic acid) (PLGA) porous scaffolds, using 3D-printing technology, to overcome the shortcomings of traditional approaches. In addition, the printing parameters were critically optimized for obtaining scaffolds with normal morphology, appropriate porous architectures, and sufficient mechanical properties, for the accommodation of the bone cells. Various evaluation studies, including the exploration of mechanical properties (compressive strength and yield stress) for different thicknesses, and change of structure (printing angle) and porosity, were performed. Particularly, the degradation rate of the 3D scaffolds, printed in the optimized conditions, in the presence of hydrolytic, as well as enzymatic conditions were investigated. Their assessments were evaluated using the thermal gravimetric analyzer (TGA), differential scanning calorimetry (DSC), and gel permeation chromatography (GPC). These porous scaffolds, with their biocompatibility, biodegradation ability, and mechanical properties, have enabled the embryonic osteoblast precursor cells (MC3T3-E1), to adhere and proliferate in the porous architectures, with increasing time. The generation of highly porous 3D scaffolds, based on 3D printing technology, and their critical evaluation, through various investigations, may undoubtedly provide a reference for further investigations and guide critical optimization of scaffold fabrication, for tissue regeneration.


2020 ◽  
Vol 315 ◽  
pp. 113778
Author(s):  
Abderrahim Titi ◽  
Saud M. Almutairi ◽  
Abdulwahed F. Alrefaei ◽  
Salim Manoharadas ◽  
Bakheet A. Alqurashy ◽  
...  

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