Synthesis of novel star-shaped molecules based on a pentaerythritol core linked to different heterocyclic systems

Diab, Hadeer M.; Abdelhamid, Ismail A.; Salem, Mostafa E.; Ragab, Islam; Zaki, Magdi E.A.; Abdelmoniem, Amr M.; Elwahy, Ahmed H.M.

doi:10.1016/j.rechem.2024.101726

Results in Chemistry

2024

DOI: 10.1016/j.rechem.2024.101726

|View full text |Cite

Synthesis of novel star-shaped molecules based on a pentaerythritol core linked to different heterocyclic systems

Hadeer M. Diab,

Ismail A. Abdelhamid,

Mostafa E. Salem

et al.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2024

2025

Publication Types

Select...

Article2

Relationship

Self Cite0

Independent2

Authors

Journals

Cited by 2 publications

References 77 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

New cyano-acrylamide derivatives incorporating the thiophene moiety: Synthesis, anti-cancer, gene expression, DNA fragmentation, DNA damage, and in silico studies

Sroor,

Elhakim,

Abdelrehim

et al. 2025

Journal of Molecular Structure

View full text Add to dashboard Cite

New cyano-acrylamide derivatives incorporating the thiophene moiety: Synthesis, anti-cancer, gene expression, DNA fragmentation, DNA damage, and in silico studies

Sroor,

Elhakim,

Abdelrehim

et al. 2025

Journal of Molecular Structure

View full text Add to dashboard Cite

Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

Abdelaal,

Ragheb,

Hassaneen

et al. 2024

Sci Rep

View full text Add to dashboard Cite

A novel series of six [1,2,4]triazolo[3,4- a ]isoquinolin-3-yl)-3-(1,3-diphenyl-1 H -pyrazol-4-yl)prop-2-en-1-ones ( 3a – 3f ) was designed and synthesized. They were characterized based on spectral and elemental analyses. In silico studies were also committed to provide insights and a better understanding of their structural features. The six compounds were screened for their antiproliferative activity using the MTT assay against five human cancer cell lines, namely, A549, HCT116, PC3, HT29, and MCF-7 in parallel with the non-cancerous human lung cell line WI-38. The results showed that 3e and 3f have potential cytotoxic activities, especially on A549 cells with IC 50 = 2.3 µM and 1.15 µM, respectively. Meanwhile, they recorded a minimal cytotoxic effect on WI-38 cells. Concerning the molecular mechanism of action, the present study showed the inhibitory effect of the six compounds against total EGFR. The most potent EGFR inhibitors were 3e and 3f with IC 50 = 0.031 µM and 0.023 µM, respectively. The selectivity index of 3f for EGFR T790M was 1.81 times more selective than that of lapatinib. In addition, 3e and 3f initiated cell cycle arrest at the G2/M and pre-G1 phases along with the downregulation of anti-apoptotic protein Bcl2 and the upregulation of pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. Further studies are recommended to evaluate animal models’ promising anticancer activity and molecular mechanism of triazolo[3,4- a ]isoquinoline derivatives 3e and 3f . Supplementary Information The online version contains supplementary material available at 10.1038/s41598-024-76459-x.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Synthesis of novel star-shaped molecules based on a pentaerythritol core linked to different heterocyclic systems

Cited by 2 publications

References 77 publications

New cyano-acrylamide derivatives incorporating the thiophene moiety: Synthesis, anti-cancer, gene expression, DNA fragmentation, DNA damage, and in silico studies

New cyano-acrylamide derivatives incorporating the thiophene moiety: Synthesis, anti-cancer, gene expression, DNA fragmentation, DNA damage, and in silico studies

Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer

Contact Info

Product

Resources

About