13754-38-6Relevant articles and documents
Design, synthesis and antitumor evaluation of new 1,8-naphthalimide derivatives targeting nuclear DNA
Liang, Gui-Bin,Wei, Jian-Hua,Jiang, Hong,Huang, Ri-Zhen,Qin, Jing-Ting,Wang, Hui-Ling,Wang, Heng-Shan,Zhang, Ye
, (2021)
Four series of new 3-nitro naphthalimides derivatives, 4(4a?4f), 5(5a?5i), 6(6a?6e) and 7 (7a?7j), were designed and synthesized as antitumor agents. Methyl thiazolyl tetrazolium (MTT) screening assay results revealed that some compounds displayed effecti
Design, synthesis, and biological evaluation of matrine derivatives possessing piperazine moiety as antitumor agents
Xu, Yiming,Liang, Pengyun,Rashid, Haroon ur,Wu, Lichuan,Xie, Peng,Wang, Haodong,Zhang, Shuyan,Wang, Lisheng,Jiang, Jun
, p. 1618 - 1627 (2019)
Using matrine (1) as the lead compound, a series of new piperazinyl matrine derivatives were designed, synthesized and evaluated for their antitumor activities in vitro and in vivo. Structure activity relationship (SAR) analysis indicated that introductio
Novel D2/5-HT receptor modulators related to cariprazine with potential implication to schizophrenia treatment
Bojarski, Andrzej J.,Dehaen, Wim,Janousek, Jiri,Juza, Radomir,Karasova, Jana Zdarova,Kobrlova, Tereza,Korabecny, Jan,Kubacka, Monika,Mezeiova, Eva,Mogilski, Szczepan,Musilek, Kamil,Pejchal, Jaroslav,Petrasek, Tomas,Prchal, Lukas,Randakova, Alena,Satala, Grzegorz,Soukup, Ondrej,Stark, Holger,Stefkova-Mazochova, Kristyna,Svozil, Daniel,Vlcek, Premysl,Vojtechova, Iveta
supporting information, (2022/02/17)
Schizophrenia is a serious mental disorder without a fully understood pathomechanism, but which involves dysregulation of neurotransmitters and their receptors. The best option for the management of schizophrenia comprises so-called multi-target ligands, similar to the third generation of neuroleptics. Dopamine type 2 receptors (D2Rs) are the main target in the treatment of schizophrenia, in particular for mitigation of the positive symptoms. Due to the high expression of 5-hydroxytryptamine type 3 receptors (5-HT3Rs) in human brain areas responsible for emotional behavior, motivation, and cognitive function, 5-HT3Rs represent a potential target for modulating the cognitive and negative symptoms of schizophrenia. Here we present the design, synthesis, and both in vitro and in vivo biological evaluation of 1,4-disubstituted aromatic piperazines. Screening of in vitro properties revealed the two most promising drug candidates (21 and 24) which were found to be potent D2Rs and moderate 5-HT3R antagonists, and which were forwarded to in vivo studies in Wistar rats. Considering toxicity, administration of the maximal feasible dose of 21 (2 mg/kg) did not produce any side effects. By contrast, the higher solubility of 24 led to revelation of mild and temporary side effects at the dose of 20 mg/kg. Importantly, both 21 and 24 showed facile crossing of the blood-brain barrier, even exerting higher levels in the brain in comparison to plasma. In a behavioral study using the acute amphetamine model of psychosis, we showed that compound 24 ameliorated both positive and negative effects of amphetamine including hyperlocomotion, social impairments, and disruption of prepulse inhibition. The effect of the highest dose (10 mg/kg) was comparable to the effect of the reference dose of aripiprazole (1 mg/kg).
Anti-tumor compound, pharmaceutically acceptable salt, preparation method and application thereof
-
, (2021/03/13)
The invention provides an anti-tumor compound and the pharmaceutically acceptable salt thereof, which have good anti-breast cancer activity, are excellent anti-breast cancer lead compounds, and have broad prospects in preparation of drugs for preventing or treating breast cancer. The preparation method is simple and convenient for industrial production.
