Anti-Cancer and Kinases Inhibitor Activities of Synthesized Heterocyclic Substituted Thiophene Fused with Cyclohexane Derivatives

Author:

Amr Abd El-Galil E1,Ghanem Hassan Z2,Al-Omar Mohamed A1,Abdalla Mohamed M3,Assy Mohamed G4,Ragab Islam4

Affiliation:

1. Pharmaceutical Chemistry Department, Drug Exploration and Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia

2. Theripeutical Chemistry Department, National Research Centre, 12622-Dokki, Cairo, Egypt

3. Research Unit, Saco Pharm. Co., 6th October City 11632, Egypt

4. Department of Chemistry, Faculty of Science, Zagazig University, Zagazig 12435, Egypt

Abstract

We herein report the anti-cancer and kinases inhibitor activities of some synthesized heterocyclic substituted thiophene fused with cyclohexane derivatives (Fig. 1) were synthesized before. Sixteen of these compounds were conveniently screened for their in vitro cytotoxicity against a wide range of cell lines, and showed potent activities against lung and leukemic cancer cell lines. The in vivo antilung and antileukemic cancers of the most active in vitro compounds was estimated and founded highly potent and compared to the standard drugs Bevacizumab and Etoposide. In search for the mechanism of action of anticancer activities it was found that these compounds exert its action via sphingosine kinase inhibition and inhibition of p53 ubiquitination.

Publisher

American Scientific Publishers

Subject

Electrical and Electronic Engineering,Computational Mathematics,Condensed Matter Physics,General Materials Science,General Chemistry

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