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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)乙酰胺的合成及体外细胞毒性评估

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.

作者信息

Aliabadi Alireza, Hasanvand Zaman, Kiani Amir, Mirabdali Seyed Saber

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.

Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran. ; Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran.

出版信息

Iran J Pharm Res. 2013 Fall;12(4):687-93.

Abstract

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.

摘要

癌症是全球第二大致死原因。尽管在诊断和治疗方面取得了进展,但患者的总体生存率仍然很低。因此,迫切需要开发新的抗癌药物。考虑到1,3,4-噻二唑衍生物具有良好的生物活性,本研究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核磁共振、红外光谱和质谱等光谱方法进行了表征。MTT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。苯环上带有间甲氧基的化合物3g是该系列中最有效的,其对MDA乳腺癌细胞系的IC50 = 9 μM,而作为参考药物的伊马替尼的IC50 = 20 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2322/3904016/437f17bfccb7/ijpr-12-687-g001.jpg

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