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Antimicrobial, Antitumor and Side Effects Assessment of a Newly Synthesized Tamoxifen Analog

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Background: Tamoxifen citrate is a very prevalent drug marketed under several trade names like Apo-Tamox, Nolvadex, Tamec, Tamizam, and Tamoplex. This molecule is approved by the FDA for breast cancer treatment. Some studies have shown that tamoxifen has anti-tuberculosis and antiparasitic activities. Like any drug, tamoxifen possesses side effects, more or less dangerous.

Aims: Basically, this work is a comparative study that aims to: primarily compare the antimicrobial and antitumor activities of tamoxifen and a newly synthesized tamoxifen analog; and to determine the molecule with lesser side effects.

Methods: Three groups of mice were injected with tamoxifen citrate and compound 2(1,1-bis[4-(3- dimethylaminopropoxy)phenyl]-2-phenyl-but-1-ene dihydrochloride) at doses corresponding to C1 (1/10), C2 (1/50), and C3 (1/100) to compound 2 lethal dose (LD50 = 75 mg/kg) administered to adult mice. A group of noninjected mice served as a study control.

Results: Experimental results suggest that compound 2 has better antitumor and antimicrobial activity than tamoxifen citrate besides its lower toxicity effects.

Conclusion: The results obtained from the present study confirmed the antitumor and antimicrobial effect of tamoxifen citrate and its hematological side effects. Compound 2 seems to be more effective than tamoxifen citrate for antitumor and antimicrobial treatment while having less hematological side effects and less disruption of the blood biochemical parameters. These findings encourage us to perform further studies on compound 2 and test it for other therapeutic uses for which tamoxifen was found effective.
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Keywords: 1;1-bis[4-(3-dimethylaminopropoxy)phenyl]-2-phenyl-but-1-ene dihydrochloride; Antimicrobial activity; Antitumor; Mice; Tamoxifen citrate; Toxicity

Affiliations: 1: Centre of Biotechnology of Sfax, University of Sfax, Route de Sidi Mansour km 6, 3018 Sfax, Tunisia. 2: Institut Supérieur de Biotechnologie de Sfax, Université de Sfax, Route de Sokra km 4, 3000 Sfax, Tunisia. 3: Faculty of Medicine, University of Sfax, Laboratory of Pharmacology UR/12 ES-13, 3029 Sfax, Tunisia. 4: Sorbonne Université, UMR 8232 CNRS, IPCM, 4 place Jussieu, F-75005 Paris (France). 5: PSL, Chimie ParisTech, 11 rue Pierre et Marie Curie, F- 75005 Paris (France). 6: School of Nutrition Sciences, University of Ottawa, Ottawa, K1N 7 K4, ON, Canada. 7: Departemt of Pharmaceutical Chemistry, Sri Sai College of Pharmacy, Badhani, Pathankot-145001, Punjab, India.

Appeared or available online: September 3, 2020

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