87539-85-3Relevant academic research and scientific papers
3,6-substituted -1, 2, 4-triazole [3,4-a] [...] compound and its preparation and use
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Paragraph 0093-0095, (2017/02/02)
The invention belongs to the field of medicinal chemistry, and discloses a 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound having antitumor activity as well as a synthesizing method and application of the 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound. The 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound has a structure as shown in a general formula I, wherein R1 refers to H, methyl or phenyl; R2 refers to 4-fluorophenyl, 4-chloroanilino, 4-bromophenyl, 4-methoxyphenyl, 4-hydroxydiphenyl, 2-fluorophenyl, 3-trifluoromethyl)phenyl]amino, naphthylamine-1-yl, pyrrolidone-1-yl, piperidine-1-yl, 3,5-dimethyl piperidine-1-yl, morpholine-4-yl, or piperazidine-1-yl. The preliminary in-vitro antitumor activity finds that the serial compounds have obvious inhibit and killing effects on multiple tumor cells, and the 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound can act as an active ingredient to be applied to clinical prevention and cancer treatment after being developed into a novel medicament.
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.
6-(Alkylamino)-3-aryl-1,2,4-triazolophthalazines. A New Class of Benzodiazepine Receptor Ligands
Tarzia, Giorgio,Occelli, Emilio,Toja, Emilio,Barone, Domenico,Corsico, Nerina,et al.
, p. 1115 - 1123 (2007/10/02)
Some 6-(alkylamino)-3-aryl-1,2,4-triazolophthalazines have been shown to displace diazepam from rat brain specific binding sites, in vitro, with Ki (nM) values comparable to those of reference benzodiazepines and to have anticonvulsant (
