Radiosynthesis and Preclinical Evaluation of [99mTc]Tc-Tigecycline Radiopharmaceutical to Diagnose Bacterial Infections DOI Creative Commons

Syeda Marab Saleem,

Tania Jabbar, Muhammad Imran

et al.

Pharmaceuticals, Journal Year: 2024, Volume and Issue: 17(10), P. 1283 - 1283

Published: Sept. 27, 2024

As a primary source of mortality and disability, bacterial infections continue to develop severe threat humanity. Nuclear medicine imaging (NMI) is known for its promising potential diagnose deep-seated infections. This work aims new technetium-99m (

Language: Английский

PROTACs: Novel tools for improving immunotherapy in cancer DOI
Shizhe Li, Ting Chen, Jinxin Liu

et al.

Cancer Letters, Journal Year: 2023, Volume and Issue: 560, P. 216128 - 216128

Published: March 16, 2023

Language: Английский

Citations

25
New Anthranilic Acid Hydrazones as Fenamate Isosteres: Synthesis, Characterization, Molecular Docking, Dynamics & in Silico ADME, in Vitro Anti‐Inflammatory and Anticancer Activity Studies DOI
Halil Şenol, Zeynep Çağman,

Tuğba Gençoğlu Katmerlikaya

et al.

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(8)

Published: June 29, 2023

In this study, twenty new anthranilic acid hydrazones 6-9 (a-e) were synthesized and their structures characterized by Fourier-transform Infrared (FT-IR), Nuclear Magnetic Resonance (1 H-NMR - 13 C-NMR), High-resolution Mass Spectroscopy (HR-MS). The inhibitory effects of the compounds against COX-II evaluated. IC50 values found in range >200-0.32 μM 6e, 8d, 8e, 9b, 9c, 9e determined to be most effective inhibitors. Cytotoxic potent investigated human hepatoblastoma (Hep-G2) healthy embryonic kidney (Hek-293) cell lines. Doxorubicin (IC50 : 8.68±0.16 for Hep-G2, 55.29±0.56 Hek-293) was used as standard. 8e is active compound, with low Hep-G2 (4.80±0.04 μM), high Hek-293 (159.30±3.12), selectivity (33.15). Finally, molecular docking dynamics studies performed understand ligand-protein interactions between COX II, Epidermal Growth Factor Receptor (EGFR), Transforming beta II (TGF-βII). scores calculated -10.609--6.705 kcal/mol COX-II, -8.652--7.743 EGFR, -10.708--8.596 TGF-βII.

Language: Английский

Citations

23
Unveiling multifunctional inhibitors: holistic spectral, electronic and molecular characterization, coupled with biological profiling of substituted pyridine derivatives against LD transpeptidase, heme oxygenase and PPAR gamma DOI Creative Commons

Shaik Yasmin Begum,

Predhanekar Mohamed Imran, Attar Kubaib

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(41), P. 29896 - 29909

Published: Jan. 1, 2024

Phenyl substituted pyridine compounds having fused pyrazole carboxylic acid derivatives.

Language: Английский

Citations

5
In vitro antiproliferative, anti-inflammatory effects and molecular docking studies of natural compounds isolated from Sarcocephalus pobeguinii (Hua ex Pobég) DOI Creative Commons
Emmanuel Mfotie Njoya,

Brigitte Ndemangou,

Jude Akinyelu

et al.

Frontiers in Pharmacology, Journal Year: 2023, Volume and Issue: 14

Published: June 21, 2023

Background:Sarcocephalus pobeguinii (Hua ex Pobég) is used in folk medicine to treat oxidative-stress related diseases, thereby warranting the investigation of its anticancer and anti-inflammatory properties. In our previous study, leaf extract S. induced significant cytotoxic effect against several cancerous cells with high selectivity indexes towards non-cancerous cells. Aim: The current study aims isolate natural compounds from pobeguinii, evaluate their cytotoxicity, effects as well searching for potential target proteins bioactive compounds. Methods: Natural were isolated leaf, fruit bark extracts chemical structures elucidated using appropriate spectroscopic methods. antiproliferative was determined on four human (MCF-7, HepG2, Caco-2 A549 cells) Vero Additionally, activity these by evaluating nitric oxide (NO) production inhibitory 15-lipoxygenase (15-LOX) activity. Furthermore, molecular docking studies carried out six putative found common signaling pathways inflammation cancer. Results: Hederagenin (2), quinovic acid 3-O-[α-D-quinovopyranoside] (6) 3-O-[β-D-quinovopyranoside] (9) exhibited all cells, they apoptosis MCF-7 increasing caspase-3/-7 showed highest efficacy poor (except cells; while (2) safety a chemotherapeutic agent. Moreover, significantly inhibited NO LPS-stimulated RAW 264.7 which could mainly be attributed effect. Besides, mixture nauclealatifoline G naucleofficine D (1), hederagenin chletric (3) active 15-LOX compared quercetin. Docking results that JAK2 COX-2, binding scores, are targets involved Conclusion: Overall, selectively killed cancer additional effect, most prominent lead compound may further investigated drug candidate tackle progression.

Language: Английский

Citations

11
Emerging COX-2 inhibitors-based nanotherapeutics for cancer diagnosis and treatment DOI

Ruiping Huang,

Yu Jiang, Baoyue Zhang

et al.

Biomaterials, Journal Year: 2024, Volume and Issue: 315, P. 122954 - 122954

Published: Nov. 7, 2024

Language: Английский

Citations

4
Optimization of pyrazole/1,2,4-triazole as dual EGFR/COX-2 inhibitors: Design, synthesis, anticancer potential, apoptosis induction and cell cycle analysis DOI

Nesma M. Kahk,

Fatma El Zahraa Ammar Mohamed,

Marwa M. Abdelhakeem

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 117340 - 117340

Published: Jan. 1, 2025

Language: Английский

Citations

0
Thiazolidinedione derivatives: emerging role in cancer therapy DOI

Ganesh Latambale,

Kapil Juvale

Molecular Diversity, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 3, 2025

Language: Английский

Citations

0
Synthesis of furan-based pyrazoline as an anticancer agent: an in vitro and in silico approach toward COX-2 inhibition DOI

Tegar Asanda Ghifari,

Fia Fathiana Wulan,

Endang Astuti

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 142125 - 142125

Published: March 1, 2025

Language: Английский

Citations

0
Drug Design and Discovery Through Artificial Intelligence DOI

Zuber Peermohammed Shaikh,

Satish Balkrishna Bhise

Advances in computational intelligence and robotics book series, Journal Year: 2025, Volume and Issue: unknown, P. 141 - 168

Published: March 7, 2025

The pharmaceutical industry has seen a create powerful in data digitization past few years. However, challenge of gathering, evaluating, and utilizing knowledge to solve complicated. Pharmaceutical problems arises with digitalization. This encourages the usage AI, which can handle vast amounts for drug target interactions greater efficiency. Artificial intelligence (AI) is technology-based system that uses variety advanced tools networks simulate Drug Discovery Design. At same time, it does not pose complete threats human physical presence. chapter emphasizes importance artificial sector, including research development, medication repurposing, enhancing productivity, clinical trials its current future applications discovery development. To address these problems, deep learning be used generate new compounds by selecting molecules from known distribution then designing fundamental

Language: Английский

Citations

0
Unveiling structural features, chemical reactivity, and bioactivity of a newly synthesized purine derivative through crystallography and computational approaches DOI
Nadeem Abad, Shafeek Buhlak, Melek Hajji

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1311, P. 138400 - 138400

Published: April 18, 2024

Language: Английский

Citations

3