Synthesis and Antiproliferative activity in vitro of Amidino Substituted 2-phenylbenzazoles

被引:4
|
作者
Racane, Livio [1 ]
Butkovic, Kristina [2 ]
Martin-Kleiner, Irena [3 ]
Kralj, Marijeta [3 ]
Karminski-Zamola, Grace [2 ]
Hranjec, Marijana [2 ]
机构
[1] Univ Zagreb, Dept Appl Chem, Fac Text Technol, Baruna Filipovica 28a, HR-10000 Zagreb, Croatia
[2] Univ Zagreb, Fac Chem Engn & Technol, Dept Organ Chem, Marulicev Trg 20, HR-10000 Zagreb, Croatia
[3] Rudjer Boskovic Inst, Div Mol Med, Bijenicka Cesta 54,POB 180, HR-10000 Zagreb, Croatia
关键词
amidines; benzimidazoles; benzothiazoles; antiproliferative activity in vitro; DNA-BINDING; ANTITUMOR EVALUATION; BENZIMIDAZOLE; BENZOTHIAZOLE; DERIVATIVES; MODULATION;
D O I
10.5562/cca3531
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Within this work we describe the synthesis of versatile substituted 2-phenyl benzothiazole 3-10 and 2-phenylbenzimidazole 12-19 derivatives bearing amidino groups. Furthermore, the synthesized compounds were explored for their antiproliferative activity in vitro on three cancer cell lines. Tested compounds showed moderate to strong antiproliferative activity. Furthermore, the type of the attached amidino group on benzazole nuclei has the significant impact on the antiproliferative activity only within benzimidazole derivatives with 2-imidazolinyl substituted derivatives being more active in comparison to amidino substituted analogues. All obtained results revealed that this type of benzothiazole derivatives have a great potential for further optimization and development of more efficient potential antiproliferative agents.
引用
收藏
页码:181 / 189
页数:9
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