Synergetic Copper/Zinc Catalysis: Synthesis of Aryl/Heteroaryl-Fused 1H-Pyrrolo[3,2-c]pyridines

2022 ◽  
Author(s):  
Nayan Ghosh ◽  
Gayyur Rana ◽  
Shivani Choudhary ◽  
Ruchir Kant
Keyword(s):  
Biological Activity ◽  
One Step ◽  
Copper Zinc ◽  
Zinc Catalysis

The scaffolds having 1H-Pyrrolo[3,2-c]pyridine core show significant biological activity. Herein, we report a synergetic copper/zinc-catalyzed one-step annulation reaction of 2-amino (hetero)arylnitriles with ynamide-derived buta-1,3-diynes to deliver 1H-pyrrolo[3,2-c]quinoline-2,4-diamine derivatives in moderate...

The Anticoagulant Activity of 3.3’-(p-Alkylthio-Benzylidene)-Bis-4-Hydroxycoumarins and Their Oxidation Products

1967 ◽  
Vol 17 (01/02) ◽  
pp. 277-286 ◽  
Author(s):  
Maria Gumińska ◽  
M Eckstein ◽  
Barbara Stachurska ◽  
J Sulko
Keyword(s):  
Biological Activity ◽  
Anticoagulant Activity ◽  
Oxidation Products ◽  
Para Position ◽  
Sulphur Atom ◽  
Group I ◽  
One Step

SummaryThe anticoagulant activity of 3.3’-(benzylidene)-bis-4-hydroxycoumarin derivatives has been estimated by one step Quick’s method. The derivatives contained the following groups in the para position of benzylidene residue: NCS- (I), CH3-S- (II), CH3-SO-(III), CH3-S02- (IV), C2H5-S- (V), C2H5-SO- (VI), C2H5-S02- (VII). All these compounds were much more active than 3.3’-(benzylidene)-bis-4-hydroxycoumarin itself.Compounds possessing the ethyl chain at the sulphur atom (V, VI, VII) were more active than methyl homologues (II, III, IV). Comparison of the activity of the series of thio-, sulphoxy-, and sulphonyl-derivatives showed that among methyl- and ethyl-derivatives those with the sulphoxy grouping (III, VI) displayed the greatest anticoagulant activity. The action of sulphonyl (IV, VII) and thio-derivatives (II, V) was weaker and shortest. The derivative with the NCS-group (I) possessed a relatively the lowest activity among the investigated compounds. 3.3’-(p-Ethylsulphoxybenzyl-idene)-bis-4-hydroxycoumarin (VI), with distinct biological activity reached about ½ of dicoumarol activity.

One step green synthesis of hexagonal silver nanoparticles and their biological activity

2014 ◽  
Vol 20 (6) ◽  
pp. 4473-4481 ◽  
Author(s):  
Samy M. Shaban ◽  
Ismail Aiad ◽  
Mohamed M. El-Sukkary ◽  
E.A. Soliman ◽  
Moshira Y. El-Awady
Keyword(s):  
Silver Nanoparticles ◽  
Biological Activity ◽  
Green Synthesis ◽  
One Step

scholarly journals One-step FPLC-size-exclusion chromatography procedure for purification of rDMBT1 6 kb with increased biological activity

2018 ◽  
Vol 542 ◽  
pp. 16-19 ◽  
Author(s):  
Martina Tuttolomondo ◽  
Pernille Lund Hansen ◽  
Jan Mollenhauer ◽  
Henrik J. Ditzel
Keyword(s):  
Biological Activity ◽  
Size Exclusion Chromatography ◽  
Size Exclusion ◽  
Exclusion Chromatography ◽  
One Step

scholarly journals Secretory expression of the recombinant FGF-2 protein in Pichia pastoris carrying multiple copies of target gene

2020 ◽  
Vol 23 (2) ◽  
pp. First
Author(s):  
Hân Khả Lê ◽  
Nghĩa Hiếu Nguyễn ◽  
Oanh Cao Kiều Nguyễn ◽  
Nhân Trí Nguyễn
Keyword(s):  
Biological Activity ◽  
Pichia Pastoris ◽  
Cell Line ◽  
Target Gene ◽  
Promoter Sequence ◽  
Multifunctional Protein ◽  
Multiple Copies ◽  
One Step ◽  
And Migration ◽  
Nih 3T3

Introduction: Fibroblast growth factor-2 (FGF-2) is a multifunctional protein that plays an important role in the regulation of proliferation, differentiation and migration of a variety of cells. The recombinant human FGF-2 (rhFGF-2) is currently used in stem cell culture, medicine and cosmetic products. In this study, we aim to produce secreted rhFGF-2 protein from a Pichia pastoris strain containing multiple copies of the fgf-2 gene to eliminate the disadvantages of intracellular expression systems. Methods: The recombinant Pichia pastoris carrying the fgf-2 gene was cloned by using homologous cloning method. The recombinant strains were screened by PCR reactions using specific primers for the target gene and the AOX1 promoter sequence. Moreover, the copy number of the fgf-2 gene inserted into the P. pastoris genome was identified by semi-quantitative PCR method. The secreted rhFGF-2 protein was collected in the induced BMMY medium at a final methanol concentration of 0.5%, and purified by one-step heparin affinity chromatography. The quantity and biological activity of the purified protein were determined by competitive ELISA method and MTT assay on NIH-3T3 cell line, respectively. Results: Various recombinant P. pastoris clones carrying different copy numbers of the fgf-2 gene were obtained and categorized into 3 groups: the low copy strains (4-5 copies), medium copy strains (8-11 copies), and high copy strains (more than 20 copies). Among those strains, the 4-copy one produced the rhFGF-2 protein at the highest expression level. After purification, the purity of rhFGF-2 protein reached 98.8%, and the recovery yield was 179.2 µg of protein from 200 mL of flask culture (equivalent to 850 µg/L). The purified rhFGF-2 protein showed similar biological activity on NIH-3T3 cell line with the commercial FGF-2 protein. Conclusion: The recombinant FGF-2 protein was successfully secretory expressed from Pichia pastoris, and successfully purified by only one-step chromatography.

Synthesis and biological activity in GPI test of scyliorhinin I and its analogues modified in position 8 by Leu, Sar and Pro residues

1991 ◽  
Vol 56 (9) ◽  
pp. 1957-1962 ◽  
Author(s):  
Krzysztof Rolka ◽  
Gotfryd Kupryszewski ◽  
Piotr Janas ◽  
Jarosław Myszor ◽  
Zbigniew S. Herman
Keyword(s):  
Biological Activity ◽  
Guinea Pig ◽  
Solid Phase ◽  
Phase Method ◽  
Guinea Pig Ileum ◽  
Tachykinin Receptor ◽  
Solid Phase Method ◽  
One Step ◽  
Agonistic Activity ◽  
The Hill

Three analogues of scyliorhinin I with Gly in position 8 substituted with Leu, Sar and Pro residues, were synthesized by the solid-phase method. The agonistic activity was determined on isolated guinea pig ileum. Analogues with Sar and Pro in position 8 appeared to be significantly more active than scyliorhinin I and the analogues with Leu in this position. For all analogues the Hill cooperativity coefficient is much lower than one suggesting that the interaction of these peptides with tachykinin receptor(s) in not a one-step reaction.

Structural characterization of the aquaporin inhibitor 2-nicotinamido-1,3,4-thiadiazole

2015 ◽  
Vol 71 (12) ◽  
pp. 1074-1079 ◽  
Author(s):  
Marianne E. Burnett ◽  
Hannah M. Johnston ◽  
Kayla N. Green
Keyword(s):  
Biological Activity ◽  
Structural Characterization ◽  
Antimicrobial Agents ◽  
2D Nmr ◽  
Brain Barrier Permeability ◽  
Nmr Techniques ◽  
One Step ◽  
Uv Visible ◽  
The One

Nicotinamides are a class of compounds with a wide variety of applications, from use as antimicrobial agents to inhibitors of biological processes. These compounds are also cofactors, which are necessary components of metabolic processes. Structural modification gives rise to the activities observed. Similarly, 1,3,4-thiadiazoles have been shown to possess antioxidant, antimicrobial, or anti-inflammatory biological activity. To take advantage of each of the inherent characteristics of the two aforementioned functional groups, 2-nicotinamido-1,3,4-thiadiazole, C8H6N4OS, was synthesized. Since defining chemical connectivity is paramount in understanding biological activity, in this report, the structural characterization of 2-nicotinamido-1,3,4-thiadiazole has been carried out using X-ray crystallographic methods. The NMR-derived assignments were made possible by utilizing one- (1D) and two-dimensional (2D) NMR techniques. In addition, UV–Visible and IR spectroscopies, and elemental analysis were used to fully characterize the product synthesized by the one-step reaction between nicotinoyl chloride hydrochloride and 2-amino-1,3,4-thiadiazole. Computational parameters related to blood–brain barrier permeability are also presented.

Study on the Biological Activity of Anti-Tumor Peptide of Tumstatin

2011 ◽  
Vol 183-185 ◽  
pp. 1509-1512
Author(s):  
Shu Jing Wang ◽  
Ning Chen ◽  
Zhang Yi ◽  
Jia Liu ◽  
Bei Bei Xu
Keyword(s):  
Electron Microscopy ◽  
Biological Activity ◽  
Tumor Cells ◽  
Tumor Therapy ◽  
Base Sequence ◽  
Hepatocarcinoma Cell ◽  
Transmission Electron ◽  
Proliferation And Apoptosis ◽  
One Step

Tumstatin anti-tumor peptide of 19peptide can inhibit the proliferation of melanoma cell. To study its effect on the proliferation and apoptosis of different tumor cells and verify its anti-tumor non-specificity, the base sequence of 19peptide was designed and constructed engineering bacteria. The soluble 19peptide was obtained from one step chitin affinity chromatograph. By such experiment as MTT assay, cell growth curve, TUNEL assay，flow cytometry，transmission electron microscopy(TEM), the biological activity of 19peptide was studied. Experiments in vitro identified that obtained 19peptide could inhibit proliferation of hela cell and hepatocarcinoma cell. It also could promote two tumor cells apoptosis. Its anti-tumor effect will lay foundation on its mechanism of action research and clinically tumor therapy in future.

scholarly journals One-step affinity purification of fusion proteins with optimal monodispersity and biological activity: application to aggregation-prone HPV E6 proteins

2018 ◽  
Vol 17 (1) ◽  
Author(s):  
Anna Bonhoure ◽  
Auguste Demenge ◽  
Camille Kostmann ◽  
Leticia San José ◽  
Eva De la Cal ◽  
...  
Keyword(s):  
Biological Activity ◽  
Fusion Proteins ◽  
Affinity Purification ◽  
Hpv E6 ◽  
One Step
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