In vitro Antitumor, Antibacterial, and Antifungal Activities of Phenylthio-Ethyl Benzoate Derivatives
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RESEARCH ARTICLE-BIOLOGICAL SCIENCES
In vitro Antitumor, Antibacterial, and Antifungal Activities of Phenylthio-Ethyl Benzoate Derivatives Nidal Jaradat1
· Ahmad Khasati1 · Maram Hawi1 · Mohammad Qadi2 · Johnny Amer2 · Mohammed Hawash1
Received: 5 July 2020 / Accepted: 2 November 2020 © King Fahd University of Petroleum & Minerals 2020
Abstract In this study, four compounds of 2-(phenylthio)-ethyl benzoate derivatives were synthesized and evaluated for their antitumor, antibacterial, and antifungal activities. These compounds were characterized and evaluated for their cytotoxic activity in MCF7-human carcinoma cells that showed a significant decrease for compounds 2a–2d in the average of G2-M phase as 8.13 ± 1.4, 10.66 ± 1.5, 14 ± 2.2, and 3.66 ± 0.8%, respectively, compared with untreated cells (21 ± 2%; p < 0.05). The data suggest that 2d compound could have an anticancer potential in the G2-M phase arrest of MCF-7 cells ultimately leading to necrosis. The compounds were tested for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, Proteus vulgaris, Enterococcus faecium, Pseudomonas aeruginosa, MRSA, and Candida albicans and showed antimicrobial potential with MIC value average (3.125–6.25 mg/ml), compared with ampicillin (0.001–3.125 mg/ml). When the MIC of the four compounds was compared with known references, we found that the 2a compound has the same MIC as fluconazole (1.56 mg/ml), inhibitor of Candida growth. Moreover, 2a, 2b,, and 2d have the same MIC as ampicillin (3.125 mg/ml) for the inhibition of S. aureus. Keywords Benzoic acid derivatives · 2-(Phenylthio)-ethyl benzoate · Anticancer · Antibacterial · Antifungal · Ampicillin · Fluconazole
1 Introduction Cancer is considered the second leading cause of death, after heart disease. The incidence of different carcinomas is estimated to be about 10 million worldwide, and half of these – incidences are in developed countries [1, 2]. Five decades of systemic drug discovery and development have led to a respectable accumulation of useful and important chemotherapeutic agents [3–5], and several important achievements in the curing and management of human cancer [6, 7]. The scientific literature shows numerous epidemiological reports that support significant differences in the occurrence of carcinoma between oriental and occidental populations [8, 9].
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Nidal Jaradat [email protected]
1
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, P.O. Box 7, 00970 Nablus, Palestine
2
Department of Biomedical Sciences, Physiology, Pharmacology and Toxicology Division, Faculty of Medicine and Health Sciences, An-Najah National University, 00970 Nablus, Palestine
Since decades, chemotherapy was the first option for cancer treatment has faced dramatic problems. Moreover, the lack of selectivity is the drawback of conventional anticancer agents, that damage not only malignant but also normal body, and blood cells have compelled scientists to develop selective and targ
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