AI Article Synopsis
- Cancer is characterized by uncontrolled cell growth, and PI3K is a key player in its progression, making it a target for new treatments.
- Researchers designed and synthesized 28 new thieno[2,3-]pyrimidine derivatives to act as anti-PI3K agents, assessing their effectiveness against different cancer cell lines.
- One compound showed significant inhibitory activity against PI3K isoforms and good cytotoxic effects, especially on breast cancer cells, suggesting it could be a promising candidate for future cancer therapies.
Article Abstract
Cancer is one of the most aggressive diseases characterised by abnormal growth and uncontrolled cell division. PI3K is a lipid kinase involved in cancer progression which makes it fruitful target for cancer control. 28 new morpholine based thieno[2,3-] pyrimidine derivatives were designed and synthesised as anti-PI3K agents maintaining the common pharmacophoric features of several potent PI3K inhibitors. Their antiproliferative activity on NCI 60 cell lines as well as their enzymatic activity against PI3K isoforms were evaluated. Three compounds revealed good cytotoxic activities against breast cancer cell lines, especially T-47D. Compound exhibited the best enzymatic inhibitory activity (72% & 84% on PI3Kβ & PI3Kγ), respectively and good activity on most NCI cell lines especially those with over expressed PI3K. Docking was carried out into PI3K active site which showed comparable binding mode to that of the PI-103 inhibitor. Compound could be optimised to serve as a new chemical entity for discovering new anticancer agents.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8725920 | PMC |
| http://dx.doi.org/10.1080/14756366.2021.2010729 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!