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Design, synthesis and biological evaluation of novel arylidine-malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B
Springer Science and Business Media LLC - - 2013
In this study, we describe the design, synthesis, biological evaluation and molecular modelling studies of novel non-carboxylic arylidine malononitrile-based molecules as Protein Tyrosine Phosphatase 1B (PTP1B) inhibitors. The synthesized derivatives were evaluated in vitro for glucose reuptake using L6 muscle cell lines and enzymatic assay against PTP1B. The biological activity results showed tha......
In vitro production of reactive oxygen species (ROS) by sampangine
Springer Science and Business Media LLC - Tập 26 Số 6 - Trang 1170-1175 - 2017
Sampangine is an azaoxoaporphine alkaloid with interesting biological activities. Elucidating the mode of action of sampangine is a topic of continuous research. Recently reported cell-based data have indicated heme-dysfunction and subsequent reactive oxygen species production as being responsible for the biological activity of the natural product. By using an in vitro biochemical assay the abilit......
In vitro antiproliferative activity of 11-aminoalkylamino-substituted 5H-indolo[2,3-b]quinolines; improving activity of neocryptolepines by installation of ester substituent
Springer Science and Business Media LLC - Tập 22 - Trang 4492-4504 - 2013
The research article describes the effect of an ester group on the in vitro antiproliferative activity in SAR studies of 5-methyl-5H-indolo[2,3-b]quinoline (neocryptolepine) derivatives. The C-2 and/or C-9 ester-substituted neocryptolepines were synthesized starting from indole-3-carboxylates and N-methylanilines, which were bearing an ester group. To these ester-substituted neocryptolepines, vari......
N, N’-disubstitutedphenyl-4-ethoxyl benzene-1, 3-disulfonamides: design, synthesis, and evaluation of anti-platelet aggregation activity
Springer Science and Business Media LLC - Tập 28 - Trang 1388-1401 - 2019
According to the bio-isosterism theory, a series of N, N’-disubstitutedphenyl-4-ethoxylbenzene-1, 3-disulfonamides (5a-p) were designed and synthesized by two steps of reactions including chlorosulfonation and ammonolysis. The structures of all compounds have been confirmed by IR, 1H-NMR, 13C-NMR, and ESI-MS spectra. The in vitro anti-platelet aggregation activities were evaluated by Born’s test i......
Ligand-based 3D-QSAR analysis and virtual screening in exploration of new scaffolds as Plasmodium falciparum glutathione reductase inhibitors
Springer Science and Business Media LLC - Tập 23 - Trang 25-33 - 2013
Plasmodium falciparum glutathione reductases involved in redox homeostasis pathway of parasite are found to be the most emerging target in the treatment of malaria. In the present study, a 3D-QSAR pharmacophore model was developed, based on twenty-three 1,4-naphthoquinone derivatives reported previously with marked inhibition against glutathione reductase (GR). The pharmac......
Three-dimensional quantitative structure–activity relationship (3D-QSAR) analysis and molecular docking of ATP-competitive triazine analogs of human mTOR inhibitors
Springer Science and Business Media LLC - Tập 21 - Trang 1207-1217 - 2011
The mTOR (mammalian target of rapamycin), a serine/threonine kinase has been identified as an important target for cancer. A 3D-QSAR analysis was carried out on 40 triazine based analogs of ATP-competitive mTOR kinase inhibitors. The study includes molecular field analysis (MFA) with G/PLS to predict the steric and electrostatic molecular field requirement for the activity of inhibitors. The QSAR ......
Computational evaluation and experimental in vitro antibacterial, antifungal and antiviral activity of bis-Schiff bases of isatin and its derivatives
Springer Science and Business Media LLC - - 2013
Design, synthesis and anticancer activities of halogenated Phenstatin analogs as microtubule destabilizing agent
Springer Science and Business Media LLC - Tập 28 - Trang 465-472 - 2019
A series of halogenated Phenstatin analogs were designed as microtubule destabilizing agent by docking study. It was synthesized within three steps starting from 2-chloro-5-iodobenzoic acid and substituted benzene. All the products were characterized by 1H NMR and 13C NMR spectral analysis, and the stereochemical structure was also confirmed by a single crystal X-ray diffraction crystallographic a......
Study of solvent effects on structural and conformational properties of cimetidine tautomers
Springer Science and Business Media LLC - Tập 25 - Trang 2042-2057 - 2016
One of the members of a class of medications is cimetidine that is called H2-receptor antagonist or H2 blockers. Cimetidine reduced the amount of acid secreted by the lining cells of the stomach. It is commonly used in treatment of gastro-esophageal reflux disease and peptic ulcer disease. In this study, the cimetidine’s tautomers stability, structural data, HOMO, LUMO orbitals (energies and shape......
Synthesis of (substituted benzamidostyryl) lH-benzimidazoles and their screening for anti-inflammatory activity
Springer Science and Business Media LLC - Tập 21 - Trang 459-467 - 2011
A series of substituted (benzamidostyryl) benzimidazole (3a–r) were synthesized and evaluated for their possible anti-inflammatory and ulcerogenicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Majority of the compounds were active in carrageenan-induced hind paw edema method test and compounds 3b, 3k had shown high potenc......
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