Synthesis, Characterization, and Anticancer Activity of New Quinazoline Derivatives against MCF-7 Cells

Author:

Faraj Fadhil Lafta12,Zahedifard Maryam3,Paydar Mohammadjavad4,Looi Chung Yeng4,Abdul Majid Nazia3,Ali Hapipah Mohd1,Ahmad Noraini1,Gwaram Nura Suleiman1,Abdulla Mahmood Ameen5

Affiliation:

1. Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia

2. Department of Chemistry, Faculty of Science, University of Diyala, Diyala Governorate, Iraq

3. Institute of Biological Sciences, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia

4. Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia

5. Department of Biomedical Science, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia

Abstract

Two new synthesized and characterized quinazoline Schiff bases 1 and 2 were investigated for anticancer activity against MCF-7 human breast cancer cell line. Compounds 1 and 2 demonstrated a remarkable antiproliferative effect, with an IC50value of 6.246 × 10−6mol/L and 5.910 × 10−6mol/L, respectively, after 72 hours of treatment. Most apoptosis morphological features in treated MCF-7 cells were observed by AO/PI staining. The results of cell cycle analysis indicate that compounds did not induce S and M phase arrest in cell after 24 hours of treatment. Furthermore, MCF-7 cells treated with 1 and 2 subjected to apoptosis death, as exhibited by perturbation of mitochondrial membrane potential and cytochrome c release as well as increase in ROS formation. We also found activation of caspases-3/7, -8, and -9 in compounds 1 and 2. Moreover, inhibition of NF-κB translocation in MCF-7 cells treated by compound 1 significantly exhibited the association of extrinsic apoptosis pathway. Acute toxicity results demonstrated the nontoxic nature of the compounds in mice. Our results showed significant activity towards MCF-7 cells via either intrinsic or extrinsic mitochondrial pathway and are potential candidate for furtherin vivoand clinical breast cancer studies.

Funder

Universiti Malaya

Publisher

Hindawi Limited

Subject

General Environmental Science,General Biochemistry, Genetics and Molecular Biology,General Medicine

Reference44 articles.

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