| Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety | |
| Alternative Title | Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety |
| Huang Qiang; Fu Qiangqiang; Liu Yajing; Bai Jinying; Wang Qianying; Liao Huimin; Gong Ping | |
| 2014 | |
| Source Publication | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
 |
| ISSN | 1005-9040 |
| Volume | 30Issue:2Pages:257-265 |
| Abstract | In an attempt to develop potent and selective anticancer agents, we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives bearing aylmethylene hydrazine moiety and evaluated their cytotoxicity, in vitro, against H460(non-small-cell lung cancer), HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines. The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1, and six target compounds(7e, 7h, 7j, 9a, 9b, 9c) were superior to PAC-1 against all the tested cancer cell lines. The most active compound 7j, with IC50(inhibitory concentration 50%) values of 0.75, 0.34 and 0.60 mu mol/L against HT-29, H460 and MDA-MB-231 cancer cell lines, was 39-, 28-, and 60-fold more potent than BMCL-200908069-1(29.24, 9.52 and 36.21 mu mol/L), respectively. |
| Other Abstract | In an attempt to develop potent and selective anticancer agents, we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives bearing aylmethylene hydrazine moiety and evaluated their cytotoxicity, in vitro, against H460(non-small-cell lung cancer), HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines. The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1, and six target compounds(7e, 7h, 7j, 9a, 9b, 9c) were superior to PAC-1 against all the tested cancer cell lines. The most active compound 7j, with IC_(50)(inhibitory concentration 50%) values of 0.75, 0.34 and 0.60 μmol/L against HT-29, H460 and MDA-MB-231 cancer cell lines, was 39-, 28-, and 60-fold more potent than BMCL-200908069-1(29.24, 9.52 and 36.21 μmol/L), respectively. |
| Keyword | POTENTIAL ANTITUMOR AGENTS BIOLOGICAL EVALUATION INHIBITOR MTOR Bis(morpholino-1,3,5-triazine) Design Anticancer activity |
| Indexed By | CSCD |
| Language | 英语 |
| Funding Project | [Program for Innovative Research Team of the Ministry of Education] ; [Program for Liaoning Innovative Research Team in University, China] |
| CSCD ID | CSCD:5111876 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/147503 |
| Collection | 中国科学院金属研究所 |
| Affiliation | 中国科学院金属研究所 |
| Recommended Citation GB/T 7714 | Huang Qiang,Fu Qiangqiang,Liu Yajing,et al. Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2014,30(2):257-265. |
| APA | Huang Qiang.,Fu Qiangqiang.,Liu Yajing.,Bai Jinying.,Wang Qianying.,...&Gong Ping.(2014).Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,30(2),257-265. |
| MLA | Huang Qiang,et al."Design, Synthesis and Anticancer Activity of Novel 6-(Aminophenyl)-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 30.2(2014):257-265. |
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