Pyridine ‐substituted thiazolylphenol derivatives: Synthesis, modeling studies, aromatase inhibition, and antiproliferative activity evaluation
In this study, pyridine‐substituted thiazolylphenol derivatives, which are non‐steroidal triazole bioisosteres, were synthesized using the Hantzsch method, and physical analysis and structural determination studies were performed. The IC50 values of the compounds were determined by a fluorescence‐based aromatase inhibition assay. Then, their antiproliferative activities on the MCF7 and HEK 293 cell lines were evaluated with the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. Furthermore, the crystal structure of human placental aromatase was subjected to a series of docking exper...
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Authors: Merve Ertas, Zafer Sahin, Barkin Berk, Leyla Yurttas, Sevde N. Biltekin, Seref Demirayak Tags: FULL PAPER Source Type: research
Synthesis, p38 α MAP kinase inhibition, anti‐inflammatory activity, and molecular docking studies of 1,2,4‐triazole‐based benzothiazole‐2‐amines
Abstract
Recent studies have demonstrated that inhibition of p38α MAP kinase could effectively inhibit pro‐inflammatory cytokines including TNF‐α and interleukins. Thus, inhibition of this enzyme can prove greatly beneficial in the therapy of chronic inflammatory diseases. A new series of N‐[3‐(substituted‐4H‐1,2,4‐triazol‐4‐yl)]‐benzo[d]thiazol‐2‐amines (4a–n) were synthesized and subjected to in vitro evaluation for anti‐inflammatory activity (BSA anti‐denaturation assay) and p38α MAPK inhibition. Among the compounds selected for in vivo screening of anti‐inflammatory activity (4b, 4c, ...
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Authors: Sana Tariq, Ozair Alam, Mohammad Amir Tags: FULL PAPER Source Type: research
Synthesis, docking, in vitro and in vivo antidiabetic activity of pyrazole ‐based 2,4‐thiazolidinedione derivatives as PPAR‐γ modulators
Abstract
The design, synthesis, structure–activity relationship, and biological activity of 2,4‐thiazolidinedione derivatives as peroxisome proliferator‐activated receptor‐γ (PPAR‐γ) modulators for antidiabetic activity are reported. Fifteen 2,4‐thiazolidinedione derivatives clubbed with pyrazole moiety were docked into the ligand binding domain of PPAR‐γ by the Glide XP module of Schrodinger. Eight derivatives (5a, 5b, 5d, 5f, 5i, 5l, 5n, 5o) having Glide XP scores > −8 as compared to the standard drug, rosiglitazone (Glide XP score = −9.165), showed almost similar interaction with the amin...
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Authors: Mohd. Javed Naim, Ozair Alam, Md. Jahangir Alam, Mohammad Shaquiquzzaman, Md. Mumtaz Alam, Vegi Ganga Modi Naidu Tags: FULL PAPER Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (2/2018)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Tags: EDITORIAL BOARD Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (2/2018)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Tags: COVER PICTURE Source Type: research
Biological evaluation and pharmacophore modeling of some benzoxazoles and their possible metabolites
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 23, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 23, 2018 Category: Drugs & Pharmacology Source Type: research
Design, synthesis, and evaluation of new α‐aminonitrile‐based benzimidazole biomolecules as potent antimicrobial and antitubercular agents
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 22, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 22, 2018 Category: Drugs & Pharmacology Source Type: research
Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 11, 2018 Category: Drugs & Pharmacology Source Type: research
Design, synthesis, and molecular docking of novel indole scaffold ‐based VEGFR‐2 inhibitors as targeted anticancer agents
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 11, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 11, 2018 Category: Drugs & Pharmacology Source Type: research
Design, synthesis, and molecular docking of novel indole scaffold ‐based VEGFR‐2 inhibitors as targeted anticancer agents
Abstract
A series of new indole derivatives 1–18 was synthesized and tested for their cytotoxic activity on a panel of 60 tumor cell lines. Additionally, molecular docking was carried out to study their binding pattern and binding affinity in the VEGFR‐2 active site using sorafenib as a reference VEGFR‐2 inhibitor. Based on the molecular docking results, compounds 5a, 5b, 6, 7, 14b, 18b, and 18c were selected to be evaluated for their VEGFR‐2 inhibitory activity. Compound 18b exhibited a broad‐spectrum antiproliferative activity on 47 cell lines, with GI % ranging from 31 to 82.5%. Moreover, compound 18b was the ...
Source: Archiv der Pharmazie - January 11, 2018 Category: Drugs & Pharmacology Authors: Hanaa M. Roaiah, Iman A. Y. Ghannam, Islam H. Ali, Ahmed M. El Kerdawy, Mamdouh M. Ali, Safinaz E ‐S. Abbas, Sally S. El‐Nakkady Tags: FULL PAPER Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (1/2018)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - January 3, 2018 Category: Drugs & Pharmacology Tags: EDITORIAL BOARD Source Type: research
