Synthesis and antitumor activity of novel 6-substituted methylenehydrazinyl-2,4-bismorpholino-pyrimidine and 1,3,5-triazine derivatives was written by Cao, Yun-yun;Zhu, Wu-fu;Zhu, Yan;Guo, Fei;Lu, Xiang-ran;Gong, Ping. And the article was included in Zhongguo Yaowu Huaxue Zazhi in 2013.Related Products of 774-47-0 This article mentions the following:
A series of 6-substituted methylenehydrazinyl-2,4-bismorpholino-pyrimidine and 1,3,5-triazine derivatives were synthesized and their chem. structures were confirmed by 1H-NMR and MS spectra. As the raw materials, 2,4,6-trichloropyrimidine or cyanuric chloride, aniline, benzimidazole and pyrrole were used to obtain the title compounds by multi-step reactions including substitution, cyclization, N-alkylation and Vilsmeier reaction. All the synthesized compounds were evaluated for their antitumor activities against three cancer cell lines (H460, A549 and H226) by the MTT method and BMCL-200908069-1 as the pos. control. Most of the prepared compounds exhibited moderate cytotoxic activities and high selectivity against H460 cancer cell line and A549 compared with the pos. control compound The pharmacol. data indicated that the introduction of substituted aryl methylene group was favorable for increasing the antitumor activity. The most promising compound 6a showed a strong antitumor activity against H460, A549 and H226 cell lines with IC50 values of 3.4濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, 0.75濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1 and 0.86濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, which were 2.8 to 16.8 times more active than the pos. control (9.52濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, 29.24濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, 36.21濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1), resp. Further studies are currently underway and will be reported in the future. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0Related Products of 774-47-0).
5,6-Difluoroindoline-2,3-dione (cas: 774-47-0) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Related Products of 774-47-0
Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles