E-ISSN 2578-7322
 

Original Research 


New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh.

Abstract
Abstract
Objectives New hybrids of 4H-imidazole-4-one and imidazolidine-2,4-dione were designed, synthesized and evaluated for their antitumor activity in an attempt to reach an active antitumor agent with potentiated activity and selectivity toward cancerous cells.
Methods Compounds 10-26 and 42-61 were synthesized and tested for their in vitro antitumor activity against prostate PC-3, colorectal HCT-116, breast MCF-7 and Hela cancer cell lines, using standard MTT assay.
Key findings Compounds 12, 46 and 54 showed remarkable broad-spectrum cytotoxic potency with median IC50 nvalues of |zn|nandn|nM, respectively. Structure-activity correlation revealed that the 4-methyl group at 3-(4-methyl-phenyl)-thiazolyl function, 4-methoxy moiety on the 5-benzyl-idene group at the 4H-imidazole-4-one and un-substituted benzoyl function at position 3- of the imidazolidine-2,4-dione favor the cytotoxic activity.
Conclusions Molecular modeling study results were in-consistency with the obtained cytotoxicity results. The investigated compounds could be used as template models for further optimization.

Key words: Key-words: Synthesis, imidazolidine-2,4-dione, 4H-imidazole-4-one, Cytotoxic activity, Molecular modeling study.


 
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Pubmed Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . A J Physiol Biochem Pharmacol. 2018; 7(1): 24-41. doi:10.5455/ajpbp.20180427101802


Web Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . http://www.ajpbp.com/?mno=297824 [Access: April 24, 2019]. doi:10.5455/ajpbp.20180427101802


AMA (American Medical Association) Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . A J Physiol Biochem Pharmacol. 2018; 7(1): 24-41. doi:10.5455/ajpbp.20180427101802



Vancouver/ICMJE Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . A J Physiol Biochem Pharmacol. (2018), [cited April 24, 2019]; 7(1): 24-41. doi:10.5455/ajpbp.20180427101802



Harvard Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh (2018) New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . A J Physiol Biochem Pharmacol, 7 (1), 24-41. doi:10.5455/ajpbp.20180427101802



Turabian Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. 2018. New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . American Journal of Physiology, Biochemistry and Pharmacology, 7 (1), 24-41. doi:10.5455/ajpbp.20180427101802



Chicago Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. "New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study ." American Journal of Physiology, Biochemistry and Pharmacology 7 (2018), 24-41. doi:10.5455/ajpbp.20180427101802



MLA (The Modern Language Association) Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh. "New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study ." American Journal of Physiology, Biochemistry and Pharmacology 7.1 (2018), 24-41. Print. doi:10.5455/ajpbp.20180427101802



APA (American Psychological Association) Style

Selwan M. El-Sayed, Mahmoud B. El-Ashmawy, Said M. Bayoumi, Ghada S. Hassan, Hussein I. El-Subbagh (2018) New Imidazole-4-one and Imidazolidine-2,4-dione Analogues: Design, Synthesis, Antitumor activity and Molecular Modeling Study . American Journal of Physiology, Biochemistry and Pharmacology, 7 (1), 24-41. doi:10.5455/ajpbp.20180427101802





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