Synthesis and In-vitro Cytotoxicity Assessment of N-(5-(Benzylthio)-134- thiadiazol-2-yl)-2-(4-(trifluoromethyl)phenyl)acetamide with Potential Anticancer Activity

机译：具有潜在抗癌活性的N-（5-（苄硫基）-134-噻二唑-2-基）-2-（4-（三氟甲基）苯基）乙酰胺的合成和体外细胞毒性评估

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Cancer is the second leading cause of death in the world. Despite advances in the diagnosis and treatment, overall survival of patients still remains poor. Hence, there is an urgent need for development of new anticancer agents. Considering promising biological activity of 1,3,4-thiadiazole derivatives, in the present study, synthesis and cytotoxicity assessment of new derivatives of this ring was done. All synthesized compounds were characterized by NMR, IR and MS spectroscopic methods. Obtained data from MTT assay showed that all compounds 3a- 3l had better anticancer activity against MDA(breast cancer) compared to PC3(prostate cancer) and U87(Glioblastoma). Compound 3 g with m-OCH3 moiety on the phenyl ring was the most potent one in this series with IC50 = 9 μM against MDA breast cell line in comparison with imatinib (IC50 = 20 μM) as reference drug.

机译：癌症是世界上第二大死亡原因。尽管诊断和治疗方面取得了进步，但患者的总体存活率仍然很差。因此，迫切需要开发新的抗癌剂。考虑到1,3,4-噻二唑衍生物的有前途的生物活性，在本研究中，对该环的新衍生物进行了合成和细胞毒性评估。所有合成的化合物均通过NMR，IR和MS光谱法表征。从MTT测定法获得的数据表明，与PC3（前列腺癌）和U87（胶质母细胞瘤）相比，所有化合物3a-3l对MDA（乳腺癌）具有更好的抗癌活性。与作为参考药物的伊马替尼（IC50 = 20μM）相比，在苯环上具有m-OCH3部分的化合物3 g是该系列中最有效的化合物，对MDA乳腺癌细胞系的IC50 = 9μM。

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期刊名称 Iranian Journal of Pharmaceutical Research : IJPR
作者
Alireza Aliabadi; Zaman Hasanvand; Amir Kiani; Seyed Saber Mirabdali;
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年(卷),期 2013(12),4
年度 2013
页码 687–693
总页数 7
原文格式 PDF
正文语种
中图分类药学;
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1. Synthesis and In-vitro Cytotoxicity Assessment of N-(5-(Benzylthio)-1,3,4-thiadiazol-2-yl)-2-(4-(trifluoromethyl)phenyl)acetamide with Potential Anticancer Activity [J] . Aliabadi Alireza, Hasanvand Zaman, Kiani Amir, Iranian Journal of Pharmaceutical Research . 2013,第4期

机译：具有潜在抗癌活性的N-（5-（苄硫基）-1,3,4-噻二唑-2-基）-2-（4-（三氟甲基）苯基）乙酰胺的合成和体外细胞毒性评估
2. Synthesis, docking and cytotoxicity evaluation of N-(5-(Benzylthio)-1,3,4-thiadiazol-2-yl)-2-(3-methoxyphenyl)acetamide derivatives as tyrosine kinase inhibitors with potential anticancer activity [J] . Ahmad Mohammadi-Farani, Tayebeh Bahrami, Alireza Aliabadi Journal of Reports in Pharmaceutical Sciences . 2014,第2期

机译：N-（5-（苄硫基）-1,3,4-噻二唑-2-基）-2-（3-甲氧基苯基）乙酰胺衍生物作为酪氨酸激酶抑制剂的合成，对接和细胞毒性评估
3. Synthesis and evaluation of 2-(5-(aryl)-1,3,4-oxadiazol-2-ylthio)-N-(3-(trifluoromethyl)phenyl)acetamides and N-(4-chloro-3-fluorophenyl)-2-(5-(aryl)-1,3,4-oxadiazol-2-ylthio)acetamides as antimicrobial agents [J] . Deepkumar Joshi1, Kalpesh Parikh Journal of Chemical Sciences . 2014,第3期

机译：2-（5-（芳基）-1,3,4-恶二唑-2-基硫基）-N-（3-（三氟甲基）苯基）乙酰胺和N-（4-氯-3-氟苯基）-的合成和评价2-（5-（芳基）-1,3,4-恶二唑-2-基硫基）乙酰胺作为抗菌剂
4. Synthesis molecular docking and biological potentials of new 2-(4-(2-chloroacetyl) piperazin-1-yl)-N-(2-(4-chlorophenyl)-4-oxoquinazolin-3(4H)-yl)acetamide derivatives [O] . Shinky Mehta, Sanjiv Kumar, Rakesh Kumar Marwaha, 2019

机译：新型2-（4-（2-氯乙酰基）哌嗪-1-基）-N-（2-（4-氯苯基）-4-氧喹唑啉-3（4H）-基）乙酰胺衍生物的合成分子对接和生物潜力
5. Synthesis, Cytotoxicity Assessment and Molecular Docking of N-(5-(substituted-benzylthio)-1,3,4-thiadiazole-2-yl)-2-p-fluorophenylacetamide Derivatives as Tyrosine Kinase Inhibitors [O] . Y. Bahmani, T. Bahrami, A. Alabadi 2019

机译：作为酪氨酸激酶抑制剂的合成，细胞毒性评估和N-（5-（取代苄基硫基）-1,3,4-噻二唑-2-基氟苯乙酰胺衍生物的分子对接

Synthesis and In-vitro Cytotoxicity Assessment of N-(5-(Benzylthio)-134- thiadiazol-2-yl)-2-(4-(trifluoromethyl)phenyl)acetamide with Potential Anticancer Activity

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