ADMET profiling in drug discovery and development: perspectives of in silico, in vitro and integrated approaches
In the drug discovery setting, undesirable ADMET properties of a pharmacophore with good
predictive power obtained after a tedious drug discovery and development process may …
predictive power obtained after a tedious drug discovery and development process may …
Thiazole derivatives in medicinal chemistry: Recent advancements in synthetic strategies, structure activity relationship and pharmacological outcomes
Thiazole derivatives remains honored heterocycles in the field of medicinal chemistry. This
scaffold has been proven as a universal motif that is present in numerous pharmacologically …
scaffold has been proven as a universal motif that is present in numerous pharmacologically …
Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic …
A series of new pyrazolo-benzothiazole hybrids (7–26) were synthesised and screened for
their cytotoxic activity towards several cancer cell lines [colon (HT-29), prostate (PC-3), lung …
their cytotoxic activity towards several cancer cell lines [colon (HT-29), prostate (PC-3), lung …
Comparison of the interactions of fanetizole with pepsin and trypsin: Spectroscopic and molecular docking approach
Y Yue, Q Tu, Y Guo, Y Wang, Y Xu, Y Zhang… - Journal of Molecular …, 2022 - Elsevier
In this work, the binding affinity of fanetizole with proteases pepsin and trypsin were
investigated by spectroscopy and molecular docking. As a thiazole derivative, the …
investigated by spectroscopy and molecular docking. As a thiazole derivative, the …
A synergistic investigation of azo-thiazole derivatives incorporating thiazole moieties: a comprehensive exploration of their synthesis, characterization, computational …
In the present study, a novel series of azo-thiazole derivatives (3a–c) containing a thiazole
moiety was successfully synthesized. The structure of these derivatives was examined by …
moiety was successfully synthesized. The structure of these derivatives was examined by …
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors
AM Srour, NS Ahmed, SS Abd El-Karim… - Bioorganic & Medicinal …, 2020 - Elsevier
Heterocyclic rings such as thiazole and benzimidazole are considered as privileged
structures, since they constitute several FDA-approved drugs for cancer treatment. In this …
structures, since they constitute several FDA-approved drugs for cancer treatment. In this …
Recent advances of thiazole hybrids in biological applications
Thiazoles have attracted much synthetic interest due to their wide variety of biological
properties and are important members of heterocyclic compounds. In recent years, studies …
properties and are important members of heterocyclic compounds. In recent years, studies …
Importance of fluorine in benzazole compounds
Fluorine-containing heterocycles continue to receive considerable attention due to their
unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules …
unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules …
[HTML][HTML] Thiazole ring-the antimicrobial, anti-inflammatory, and anticancer active scaffold
S Hosseininezhad, A Ramazani - Arabian Journal of Chemistry, 2023 - Elsevier
Background Thiazole ring is one of the most important heterocycle scaffolds in organic and
medicinal chemistry due to this scaffold being the backbone of numerous drugs and their …
medicinal chemistry due to this scaffold being the backbone of numerous drugs and their …
Synthesis and biological evaluation of novel benzothiazole derivatives as potential anticonvulsant agents
DC Liu, HJ Zhang, CM Jin, ZS Quan - Molecules, 2016 - mdpi.com
New benztriazoles with a mercapto-triazole and other heterocycle substituents were
synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using the …
synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using the …