Biological evaluation of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imine derivatives.

Huang C; Yan SJ; Zeng XH; Dai XY; Zhang Y; Qing C; Lin J

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Biological evaluation of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imine derivatives.

机译：多卤代1,3-二氮杂杂环稠合的异喹啉-1（2H）-亚胺衍生物的生物学评估。

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A series of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imines were evaluated in vitro against human tumour cell lines including A431, K562, HL60, HepG2 and Skov-3. As a result, some of the target compounds such as 5b, 5c, 5i, 5o, 6c, 6h and 7f showed stronger cytotoxicity against K562, H562 and Skov-3 cells in comparison with cisplatin, and the others displayed moderate cytotoxicity to A431 and HepG2. Biological investigations using the representative compounds 5c, 6c and 6h were also performed in mice bearing S(180) and H(22) tumours. The results indicated that these three compounds inhibit S(180) and H(22) growth. In addition, compounds 6c and 6h have very low acute toxicities. The preliminary analysis of structure-activity relationships is also discussed.

机译：在体外针对人肿瘤细胞系，包括A431，K562，HL60，HepG2和Skov-3，评估了一系列多卤代1,3-二氮杂杂环稠合的异喹啉-1（2H）-亚胺。结果，与顺铂相比，某些目标化合物（例如5b，5c，5i，5o，6c，6h和7f）对K562，H562和Skov-3细胞显示出更强的细胞毒性，而其他目标化合物对A431和HepG2。使用具有代表性的化合物5c，6c和6h的生物学研究也在患有S（180）和H（22）肿瘤的小鼠中进行。结果表明这三种化合物抑制S（180）和H（22）的增长。另外，化合物6c和6h具有非常低的急性毒性。还讨论了结构-活性关系的初步分析。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第4期|共9页
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Huang C; Yan SJ; Zeng XH; Dai XY; Zhang Y; Qing C; Lin J;
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1. Biological evaluation of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imine derivatives. [J] . Huang C, Yan SJ, Zeng XH, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第4期

机译：多卤代1,3-二氮杂杂环稠合的异喹啉-1（2H）-亚胺衍生物的生物学评估。
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7. Figure 1 from: Drapak I, Zimenkovsky B, Perekhoda L, Suleyman М, Yeromina H, Skaletska N, Seredynska N, Demchenko A (2019) Search for angiotensin II receptor antagonists among 4-aryl-n-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives. Pharmacia 66(4): 181-186. https://doi.org/10.3897/pharmacia.66.e36808 [O] . Iryna Drapak, Borys Zimenkovsky, Lina Perekhoda, 2019

机译：图1来自：Drapak I，Zimenkovsky B，Perekhoda L，SuleymanМ，Yeromina H，Skaletska N，Seredynska N，Demchenko A（2019）在4-芳基-N-（芳基）-3-（芳基）中寻找血管紧张素II受体拮抗剂PROP-2-ZH-1-YL）-2,3-二氢-1,3-噻唑-2-亚胺衍生物。 Pharmacia 66（4）：181-186。 https://doi.org/10.3897/halarmacia.66.e36808

Biological evaluation of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imine derivatives.

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