Design, Synthesis, Anticancer Evaluation and In Silico Studies of Imidazole Pyrazine Compounds DOI Open Access
Gong� Chen, Weiwei Li, Liu Y

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 8, 2024

The present study focused on design and synthesis novel imidazolopyrazine derivatives, investigate the effect of them proliferation migration several human cancer cell lines by CCK-8 method, interactions with JAKs reverse molecular docking. It was found that most synthesized imidazolopyrazin derivatives exhibited excellent inhibitory effects towards three tested tutor cells in vitro. Among them, compounds have IC

Language: Английский

Benzothiazole a privileged scaffold for Cutting-Edges anticancer agents: Exploring drug design, structure-activity relationship, and docking studies DOI

I. Aayishamma,

Gurubasavaraja Swamy Purawarga Matada, Rohit Pal

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 279, P. 116831 - 116831

Published: Sept. 6, 2024

Language: Английский

Citations

8
Antitumor Effects of Tryptanthrin on Colorectal Cancer by Regulating the Mitogen-Activated Protein Kinase Signaling Pathway and Targeting Topo I and IDO1 DOI Creative Commons

Shing-Hwa Lu,

Bao-Long Hou, Ting Wang

et al.

ACS Omega, Journal Year: 2025, Volume and Issue: 10(3), P. 3206 - 3221

Published: Jan. 10, 2025

Tryptanthrin (TRYP) is an indole quinazoline alkaloid with a range of pharmaceutical activities, but the specific mechanism TRYP against colorectal cancer (CRC) remains obscure. The purpose this study was to evaluate antitumor effects on CRC models both in vitro and vivo further analyze its concrete mechanisms. results experiment show that effectively inhibited proliferation migration SW620 cells, arrested cell cycle at S phase, induced apoptosis. Deeply, dramatically increased expression Bax cleaved caspase 3 while decreasing Bcl-2. transcriptome sequencing implied inhibitory were closely related mitogen-activated protein kinase (MAPK) signaling pathway, western blotting verified could decrease p-Erk increase p-p38 p-Jnk. Besides, our identified topoisomerase I (Topo I) amine 2,3-dioxygenase 1 (IDO1) targets TRYP. In vivo, showed different doses significantly tumor growth mice, degrees necrosis tissues, decreased level Ki67 protein, apoptotic signal tissues. findings demonstrated CRC, mechanisms tightly connected inhibiting activity Topo IDO1 regulating MAPK pathway. Especially, it first directly inhibit arrest phase. Therefore, work established scientific basis for development

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
Recent advances on anticancer activity of benzodiazine heterocycles through kinase inhibition DOI Creative Commons
Mohamed S. Nafie, Sherif Ashraf Fahmy,

Shaima H. Kahwash

et al.

RSC Advances, Journal Year: 2025, Volume and Issue: 15(7), P. 5597 - 5638

Published: Jan. 1, 2025

This is an updated review for the anticancer activity of benzodiazine heterocyclic derivatives through kinase inhibition.

Language: Английский

Citations

0
Molecular docking, pharmacological profiling, and MD simulations of glycolytic inhibitors targeting novel SARS CoV-2 main protease and spike protein DOI
Nikhil Kumar,

Chandraprakash Gond,

Jai Deo Singh

et al.

In Silico Pharmacology, Journal Year: 2025, Volume and Issue: 13(1)

Published: March 14, 2025

Language: Английский

Citations

0
Late-stage functionalization of anticancer agent Daniquidone and the in vitro anticancer activities of the derivatives DOI Creative Commons

Geshuyi Chen,

Yiying Zeng, Xin Chen

et al.

European Journal of Medicinal Chemistry Reports, Journal Year: 2025, Volume and Issue: unknown, P. 100269 - 100269

Published: April 1, 2025

Language: Английский

Citations

0
Current developments in PI3K-based anticancer agents: Designing strategies, biological activity, selectivity, structure-activity correlation, and docking insight DOI

Md. Ashadul Sk,

K. Hemalatha, Gurubasavaraja Swamy Purawarga Matada

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 154, P. 108011 - 108011

Published: Nov. 29, 2024

Language: Английский

Citations

2
Advancements of anticancer agents by targeting the Hippo signalling pathway: biological activity, selectivity, docking analysis, and structure–activity relationship DOI

E Haripriya,

K. Hemalatha, Gurubasavaraja Swamy Purawarga Matada

et al.

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 22, 2024

Language: Английский

Citations

0
Bicyclic Ureas as JAK2 Inhibitors for Treating Hematological Cancer DOI Creative Commons
Ram W. Sabnis

ACS Medicinal Chemistry Letters, Journal Year: 2024, Volume and Issue: 15(11), P. 1824 - 1825

Published: Oct. 29, 2024

Provided herein are novel bicyclic ureas as JAK2 inhibitors, pharmaceutical compositions, use of such compounds in treating hematological cancer, and processes for preparing compounds.

Language: Английский

Citations

0
Design, Synthesis, Anticancer Evaluation and In Silico Studies of Imidazole Pyrazine Compounds DOI Open Access
Gong� Chen, Weiwei Li, Liu Y

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 8, 2024

The present study focused on design and synthesis novel imidazolopyrazine derivatives, investigate the effect of them proliferation migration several human cancer cell lines by CCK-8 method, interactions with JAKs reverse molecular docking. It was found that most synthesized imidazolopyrazin derivatives exhibited excellent inhibitory effects towards three tested tutor cells in vitro. Among them, compounds have IC

Language: Английский

Citations

0