Adibi Hadi, Majnooni Mohammad Bagher, Mostafaie Ali, Mansouri Kamran, Mohammadi Moslem
Novel Drug Delivery Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Student's Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran. ; Medical Biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Iran J Pharm Res. 2013 Fall;12(4):695-703.
Compounds containing triazene ring structure are cytotoxic agents and clinically used as antitumor alkylating agents. In this study, a series of triazene derivatives holding alkyl and aryl moieties were synthesized and proved to be potent cytotoxic agents in-vitro particularly against eight cancer cell lines (PC3, HT29, Hela, HL60, Jurkat, K562, MCF7, HepG2) and a non-cancerous cell line (HUVEC). The cytotoxic activity was assessed using two methods, LDH assay, and trypan blue exclusion. Some of the triazene derivatives showed cytotoxic activity more than temozolomide (TMZ) as the reference drug. The synthesized triazenes showed marked cytotoxicity effects on all eight cancer cell lines. Among the compounds synthesized, 1,3-bis(2-ethoxyphenyl)triazene C had unique efficacy and selectivity so that it had IC50 between 0.560-3.33 μM on cancer cell lines and 12.61 μM on normal cell line (HUVEC). 1-(4-nitrophenyl)-3-(2-hydroxyethyl)triazene E shows weaker effect on cancer cell lines than the other compounds having IC50 between 3-15.54 μM.
含有三氮烯环结构的化合物是细胞毒性剂，临床上用作抗肿瘤烷基化剂。在本研究中，合成了一系列含有烷基和芳基部分的三氮烯衍生物，体外实验证明它们是强效细胞毒性剂，尤其对八种癌细胞系（PC3、HT29、Hela、HL60、Jurkat、K562、MCF7、HepG2）和一种非癌细胞系（HUVEC）有效。使用两种方法评估细胞毒性活性，即乳酸脱氢酶（LDH）测定法和台盼蓝排斥法。一些三氮烯衍生物表现出比作为参考药物的替莫唑胺（TMZ）更强的细胞毒性活性。合成的三氮烯对所有八种癌细胞系均显示出明显的细胞毒性作用。在合成的化合物中，1,3-双（2-乙氧基苯基）三氮烯C具有独特的功效和选择性，其对癌细胞系的半数抑制浓度（IC50）在0.560 - 3.33μM之间，对正常细胞系（HUVEC）的IC50为12.61μM。1-（4-硝基苯基）-3-（2-羟乙基）三氮烯E对癌细胞系的作用比其他化合物弱，其IC50在3 - 15.54μM之间。
