52494-53-8Relevant articles and documents
3-substituted-6 - (1-substituted piperazinyl) - 1, 2, 4-triazole [3,4-a] [...] compound, preparation method thereof, and use thereof
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, (2016/10/08)
The invention belongs to the field of medicinal chemistry and discloses a 3-substituted-6-(1-substituted piperazinyl)-1,2,4-triazoleo[3,4-a] phthalazine compound with antitumor activity as well as a preparation method and an application thereof. The compound has a structure as shown in a general formula I, wherein in the general formula I, R1 is hydrogen, methyl or phenyl; R2 is hydrogen, 4-fluorophenyl, 4-chlorphenyl, 3-trifluoromethylphenyl or 2-fluorophenyl. The preliminary in-vitro antitumor activity evaluation proves that the series of compounds have obvious effects of inhibiting and killing multiple tumor cells. The compound can serve as an active ingredient to be developed into a novel drug and is applied to clinical prevention and cancer therapy.
Synthesis and antimicrobial activities of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives
Zhang, Qiu-Rong,Xue, Deng-Qi,He, Peng,Shao, Kun-Peng,Chen, Peng-Ju,Gu, Yi-Fei,Ren, Jing-Li,Shan, Li-Hong,Liu, Hong-Min
, p. 1236 - 1238 (2014/03/21)
A series of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives were synthesized in five steps from a common precursor, phthalic anhydride. Most of synthesized phthalazine derivatives showed inhibitory activity against Staphylococcus aureus. One of phthalazine derivatives 5l showed inhibitory activity against all tested bacterial and fungal strains.
Synthesis and anticancer activities of novel 1,2,4-triazolo[3,4-a] phthalazine derivatives
Xue, Deng-Qi,Zhang, Xu-Yao,Wang, Chao-Jie,Ma, Li-Ying,Zhu, Nan,He, Peng,Shao, Kun-Peng,Chen, Peng-Ju,Gu, Yi-Fei,Zhang, Xiao-Song,Wang, Cai-Feng,Ji, Cong-Hui,Zhang, Qiu-Rong,Liu, Hong-Min
, p. 235 - 244 (2014/08/18)
Trying to develop potent and selective anticancer agents, two series of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives were designed and synthesized. Their antitumor activities were evaluated by MTT method against four selected human cancer cell lines (MGC-803, EC-9706, HeLa and MCF-7). Our results showed that compound 11h exhibited good anticancer activities compared to 5-fluorouracil against the four tested cell lines, with IC50 values ranging from 2.0 to 4.5 μM. Flow cytometry analysis indicated that compound 11h induced the cellular early apoptosis and cell cycle arrest at G2/M phase in EC-9706.