Design, Synthesis, and Tripeptidyl Peptidase II Inhibitory Activity of a Novel Series of (S)-2,3-Dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles

2002 ◽  
Vol 45 (24) ◽  
pp. 5303-5310 ◽  
Author(s):  
Henry J. Breslin ◽  
Tamara A. Miskowski ◽  
Michael J. Kukla ◽  
William H. Leister ◽  
Hans L. De Winter ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Design Synthesis ◽  
Tripeptidyl Peptidase ◽  
Tripeptidyl Peptidase Ii

Tripeptidyl-peptidase II (TPP II) inhibitory activity of ( S )-2,3-dihydro-2-(1 H -imidazol-2-yl)-1 H -indoles, a systematic SAR evaluation. Part 2

2003 ◽  
Vol 13 (24) ◽  
pp. 4467-4471 ◽  
Author(s):  
Henry J. Breslin ◽  
Tamara A. Miskowski ◽  
Michael J. Kukla ◽  
Hans L. De Winter ◽  
Maria V.F. Somers ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Tripeptidyl Peptidase ◽  
Tripeptidyl Peptidase Ii

Tripeptidyl-Peptidase II (TPP II) Inhibitory Activity of (S)-2,3-Dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a Systematic SAR Evaluation. Part 2.

ChemInform ◽  
2004 ◽  
Vol 35 (12) ◽  
Author(s):  
Henry J. Breslin ◽  
Tamara A. Miskowski ◽  
Michael J. Kukla ◽  
Hans L. De Winter ◽  
Maria V. F. Somers ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Tripeptidyl Peptidase ◽  
Tripeptidyl Peptidase Ii

Design, Synthesis, Molecular Docking and Biological Evaluation of 1-(benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol Derivatives as Antiproliferative Agents

2019 ◽  
Vol 16 (10) ◽  
pp. 837-845
Author(s):  
Sandhya Jonnala ◽  
Bhaskar Nameta ◽  
Murthy Chavali ◽  
Rajashaker Bantu ◽  
Pallavi Choudante ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Chinese Hamster Ovary Cells ◽  
Chinese Hamster ◽  
Mouse Skin ◽  
Coupling Reaction ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Design Synthesis

A class of 1-((benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol derivatives (4a-t) has been synthesized in good yields through a three component coupling reaction. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against five cell lines such as DU145 (human prostate cancer), MDA-MB-B231 (human breast cancer), SKOV3 (human ovarian cancer), B16-F10 (mouse skin melanoma) and CHO-K1 (Chinese hamster ovary cells), a noncancerous cell line. In vitro inhibitory activity indicates that compounds 4a, 4b, 4c, 4d, 4g, 4j, and 4o exhibited potent anti-proliferative behavior. Among them, compounds 4g, 4j and 4o found to be the most active members exhibiting remarkable growth inhibitory activity. Molecular docking facilitates to investigate the probable binding mode and key active site interactions in tubulins α and β proteins. The docking results are complementary to experimental results.

Phenanthridine Sulfonamide Derivatives as Potential DPP-IV Inhibitors: Design, Synthesis and Biological Evaluation

2020 ◽  
Vol 16 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Shorooq Alqazaqi ◽  
Maram Aburezeq ◽  
Dima Sabbah ◽  
Ghadeer Albadawi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Ligand Docking ◽  
Biological Assessment ◽  
Hypoglycemic Agents ◽  
Binding Affinities ◽  
Oral Hypoglycemic Agents ◽  
Design Synthesis ◽  
Dpp Iv

Background: Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a prolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion, insulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents that reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion to stimulate the secretion of insulin from beta cells of pancreas. Objective: In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine sulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study the molecular interactions and binding affinities against DPP-IV enzyme. Methods: The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized ligand docking (QPLD) was also performed. Results: In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from 10%-46% at 100 µM concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory activity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125, E205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones. Conclusion: In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further structural optimization in order to enhance their inhibitory activity.

Investigation of a role for Glu-331 and Glu-305 in substrate binding of tripeptidyl-peptidase II

2008 ◽  
Vol 1784 (12) ◽  
pp. 1899-1907 ◽  
Author(s):  
Ann-Christin Lindås ◽  
Sandra Eriksson ◽  
Emese Jozsa ◽  
Birgitta Tomkinson
Keyword(s):  
Substrate Binding ◽  
Tripeptidyl Peptidase ◽  
Tripeptidyl Peptidase Ii

scholarly journals Tripeptidyl peptidase II serves as an alternative to impaired proteasome to maintain viral growth in the host cells

FEBS Letters ◽  
2010 ◽  
Vol 585 (1) ◽  
pp. 261-265 ◽  
Author(s):  
Jingchun Zhang ◽  
Jerry Wong ◽  
Guang Gao ◽  
Honglin Luo
Keyword(s):  
Host Cells ◽  
Viral Growth ◽  
Tripeptidyl Peptidase ◽  
Tripeptidyl Peptidase Ii
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