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Antimicrobial, Antitumor and Side Effects Assessment of a Newly Synthesized Tamoxifen Analog.
Current Topics in Medicinal Chemistry ( IF 2.9 ) Pub Date : 2020-01-01 , DOI: 10.2174/1568026620666200819145526
Fatma Abdmouleh 1 , Mehdi El Arbi 1, 2 , Hajer Ben Saad 3 , Karim Jellali 1 , Emna Ketata 1 , Ibtissem Ben Amara 2 , Pascal Pigeon 4, 5 , Hanen Ben Hassen 2 , Siden Top 4 , Gérard Jaouen 4, 5 , Riadh Hammami 6 , Mamdouh Ben Ali 1 , Girish Kumar Gupta 7
Affiliation  

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.

中文翻译:

新合成的他莫昔芬类似物的抗菌、抗肿瘤和副作用评估。

背景他莫昔芬柠檬酸盐是一种非常流行的药物,以多种商品名销售,如Apo-Tamox、Nolvadex、Tamec、Tamizam和Tamoplex。该分子已被 FDA 批准用于乳腺癌治疗。一些研究表明他莫昔芬具有抗结核和抗寄生虫活性。像任何药物一样,他莫昔芬也有副作用,或多或少是危险的。目的 基本上,这项工作是一项比较研究,旨在:主要比较他莫昔芬和新合成的他莫昔芬类似物的抗菌和抗肿瘤活性;并确定副作用较小的分子。方法 三组小鼠分别注射他莫昔芬和化合物2(1,1-双[4-(3-二甲氨基丙氧基)苯基]-2-苯基-丁-1-烯二盐酸盐)对应C1(1/10)的剂量), C2 (1/50), 和 C3 (1/100) 至化合物 2 致死剂量 (LD50 = 75 mg/kg) 给予成年小鼠。一组未注射的小鼠作为研究对照。结果实验结果表明,化合物2除毒性作用较低外,还具有比柠檬酸他莫昔芬更好的抗肿瘤和抗菌活性。结论 本研究的结果证实了柠檬酸他莫昔芬的抗肿瘤和抗菌作用及其血液学副作用。在抗肿瘤和抗微生物治疗方面,化合物 2 似乎比柠檬酸他莫昔芬更有效,同时具有更少的血液学副作用和更少的血液生化参数破坏。这些发现鼓励我们对化合物 2 进行进一步的研究,并测试它在他莫昔芬被发现有效的其他治疗用途中的作用。
更新日期:2020-08-19
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