Home|Journals|Articles by Year Follow on Twitter| Subscribe to List

Directory for Medical Articles
 

Open Access

Original Article



Synthesis and Cytotoxic Screening of Novel Spiro[Chroman-2,4'-Piperidin]-4-One Derivatives with Apoptosis-Inducing Activity

Shaimaa A. Abdelatef, Mohammed T. El-Saadi, Noha H. Amin, Ahmed H. Abdelazeem, Khaled R.A. Abdellatif.

Abstract
A novel series of spiro[chroman-2,4'-piperidin]-4-one derivatives was synthesized and evaluated as cytotoxic agents against three human cancer cell lines; MCF-7 (human breast carcinoma), A2780 (human ovarian cancer) and HT-29 (human colorectal adenocarcinoma) using MTT assay. Compound 16 with a sulfonyl spacer exhibited the most potent activity with IC50 values between 0.31 and 5.62 μM. However, the trimethoxyphenyl derivative 15 was the least potent with IC50 values between 18.77 and 47.05 μM. The most active compound 16 was selected for further mechanistic studies, which revealed that it induced more than three folds early apoptosis in MCF-7 cells treated for 24 h. Additionally, it increased MCF-7 cells in the sub-G1 and G2-M cell cycle phases, following the same treatment duration. Together, these compounds could be promising cytotoxic candidates, thus further structural optimization, in vitro and in vivo studies are recommended to be developed into potential cytotoxic agents.

Key words: Spiro[chroman-2,4'-piperidin]-4-one; cytotoxic; MTT; apoptosis; cell cycle analysis.



Full-text options

Full-text Article




Advertisement
Journal of Behavioral Health

SUBMIT YOUR ARTICLE NOW




ScopeMed.com
BiblioMed Home
Follow ScopeMed on Twitter
Author Tools
eJPort Journal Hosting
About BiblioMed
License Information
Terms & Conditions
Privacy Policy
Contact Us

The articles in Bibliomed are open access articles licensed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License (https://creativecommons.org/licenses/by-nc-sa/4.0/) which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.
ScopeMed is a Database Service for Scientific Publications. Copyright ScopeMed Information Services.