163620-93-7Relevant academic research and scientific papers
Synthesis and biological evaluation of 2,4-diaminoquinazoline derivatives as novel heat shock protein 90 inhibitors
Thorat, Dhanaji Achyutrao,Doddareddy, Munikumar Reddy,Seo, Seon Hee,Hong, Tae-Joon,Cho, Yong Seo,Hahn, Ji-Sook,Pae, Ae Nim
scheme or table, p. 1593 - 1597 (2011/05/05)
Novel 2,4-diaminoquinazoline derivatives originating from a virtual screening approach were designed, synthesized and their biological activities as heat shock protein 90 (Hsp90) inhibitors were evaluated. The prepared compounds exhibited significant anti-proliferative activities against DU-145, HT-29, HCT-116, A375P and MCF-7 cancer cell lines. The selected compounds were tested against Her2, a client protein of Hsp90, and showed significant reduction in Her2 protein expression. Compound 6b was found the most potent, reduced Her2 protein expression levels and induced Hsp70 protein expression levels significantly.
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
Kang, Suk Youn,Park, Eun-Jung,Park, Woo-Kyu,Kim, Hyun Jung,Jeong, Daeyoung,Jung, Myung Eun,Song, Kwang-Seop,Lee, Suk Ho,Seo, Hee Jeong,Kim, Min Ju,Lee, MinWoo,Han, Ho-Kyun,Son, Eun-Jung,Pae, Ae Nim,Kim, Jeongmin,Lee, Jinhwa
scheme or table, p. 1705 - 1711 (2010/06/19)
Arylpiperzine-containing pyrrole 3-carboxamide derivatives were synthesized and evaluated as novel antidepressant compounds. The various analogues were efficiently prepared and bio-assayed for binding to 5-HT2A, 5-HT2C receptor, and
Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
Kim, Jong Yup,Kim, Deukjoon,Kang, Suk Youn,Park, Woo-Kyu,Kim, Hyun Jung,Jung, Myung Eun,Son, Eun-Jung,Pae, Ae Nim,Kim, Jeongmin,Lee, Jinhwa
scheme or table, p. 6439 - 6442 (2010/11/18)
Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed.
Synthesis and biological characterization of novel hybrid 7-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro- naphthalen-2-ol and their heterocyclic bioisosteric analogues for dopamine D2 and D3 receptors
Dutta, Aloke K.,Venkataraman, Sylesh K.,Fei, Xiang-Shu,Kolhatkar, Rohit,Zhang, Shijun,Reith, Maarten E.A.
, p. 4361 - 4373 (2007/10/03)
In a recent preliminary communication we described the development of a series of hybrid molecules for the dopamine D2 and D3 receptor subtypes. The design of these compounds was based on combining pharmacophoric elements of aminotetralin and piperazine m
A novel series of hybrid compounds derived by combining 2-aminotetralin and piperazine fragments: Binding activity at D2 and D3 receptors
Dutta, Aloke K,Fei, XiangShu,Reith, Maarten E.A
, p. 619 - 622 (2007/10/03)
A series of 7-hydroxy-2-[N-alkyl-(N-(4-phenylpiperazine)-alkyl)amino]tetralins was developed based on a novel hybrid approach that combined 2-aminotetralin and arylpiperazine pharmacophoric moieties. Our preliminary study revealed that a four-methylene bu
NAPHTHALAMIDES AS CENTRAL NERVOUS SYSTEM AGENTS
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, (2008/06/13)
Naphthalamides are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as antipsychotic agents and as agents for the treatment of disorders
