152193-85-6Relevant articles and documents
Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer
Wang, Lei,Fang, Kun,Cheng, Junfei,Li, Yu,Huang, Yahui,Chen, Shuqiang,Dong, Guoqiang,Wu, Shanchao,Sheng, Chunquan
, p. 696 - 713 (2020/02/04)
Inspired by the natural product evodiamine, a novel antitumor indolopyrazinoquinazolinone scaffold was designed by scaffold hopping. Structure-activity relationship studies led to the discovery of compound 15j, which shows low nanomolar inhibitory activity against the HCT116 cell line. Further antitumor mechanism studies indicated that compound 15j acted by the dual inhibition of topoisomerase 1 and tubulin and induced apoptosis with G2 cell-cycle arrest. The quaternary ammonium salt of compound 15j (compound 15js) exhibited excellent in vivo antitumor activity (TGI = 66.6%) in the HCT116 xenograft model with low toxicity. Indolopyrazinoquinazolinone derivatives represent promising multitargeting antitumor leads for the development of novel antitumor agents.
PYRROLE mTORC INHIBITORS AND USES THEREOF
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, (2020/01/12)
The present invention provides compounds, compositions thereof, and methods of using the same.
PHENYL mTORC INHIBITORS AND USES THEREOF
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Paragraph 00443, (2018/05/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
PYRROLE mTORC INHIBITORS AND USES THEREOF
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, (2018/05/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
TRICYCLIC COMPOUNDS FOR USE IN TREATMENT OF PROLIFERATIVE DISORDERS
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, (2018/10/19)
The present invention relates to compounds of Formula (I) as defined herein, and salts, hydrates and solvates thereof. The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to the use of compounds of Formula (I) in the treatment or prevention of PRMT5-mediated disorders, such as cancer.
Efficient and general synthesis of oxazino[4,3-a]indoles by cascade addition-cyclization reactions of (1H-indol-2-yl)methanols and vinyl sulfonium salts
An, Jing,Chang, Ning-Jie,Song, Li-Dong,Jin, Yu-Qin,Ma, Ying,Chen, Jia-Rong,Xiao, Wen-Jing
supporting information; experimental part, p. 1869 - 1871 (2011/03/22)
An efficient and general approach to oxazino[4,3-a]indole architectures is described. The addition-cyclization cascade of (1H-indol-2-yl)methanols with vinyl sulfonium salts affords oxazino[4,3-a]indole derivatives in high yields.
PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
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, (2011/11/30)
Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Novel Aryl Piperazine Derivatives With Medical Utility
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Page/Page column 26; 20, (2009/10/01)
This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, D2-like and 5-HT2 receptor subtypes, and in particular u
Synthesis and pharmacological evaluation of 1,2,3,4-tetrahydropyrazino[1,2-a]indole and 2-[(phenylmethylamino)methyl]-1H-indole analogues as novel melatoninergic ligands
Markl, Christian,Attia, Mohamed I.,Julius, Justin,Sethi, Shalini,Witt-Enderby, Paula A.,Zlotos, Darius P.
experimental part, p. 4583 - 4594 (2009/12/04)
Two novel series of melatonin-derived compounds have been synthesized and pharmacologically evaluated at the MT1 and MT2 subtypes of melatonin receptors. Compounds 12b-c are non-selective high-affinity MT1 and MT2/su
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: Inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors
Campiani, Giuseppe,Butini, Stefania,Trotta, Francesco,Fattorusso, Caterina,Catalanotti, Bruno,Aiello, Francesca,Gemma, Sandra,Nacci, Vito,Novellino, Ettore,Stark, Jennifer Ann,Cagnotto, Alfredo,Fumagalli, Elena,Carnovali, Francesco,Cervo, Luigi,Mennini, Tiziana
, p. 3822 - 3839 (2007/10/03)
The synthesis, pharmacological evaluation, and structure - activity relationships (SARs) of a series of novel arylalkylpiperazines structurally related to BP897 (3) are described. In binding studies, the new derivatives were tested against a panel of dopamine, serotonin, and noradrenaline receptor subtypes. Focusing mainly on dopamine D3 receptors, SAR studies brought to light a number of structural features required for high receptor affinity and selectivity. Several heteroaromatic systems were explored for their dopamine receptor affinities, and combinations of synthesis, biology, and molecular modeling, were used to identify novel structural leads for the development of potent and selective D3 receptor ligands. Introduction of an indole ring linked to a dichlorophenylpiperazine system provided two of the most potent and selective ligands known to date (D 3 receptor affinity in the picomolar range). The intrinsic pharmacological properties of a subset of potent D3 receptor ligands were also assessed in [35S]-GTPγS binding assays. Evidence from animal studies, in particular, has highlighted the dopaminergic system's role in how environmental stimuli induce drug-seeking behavior. We therefore tested two novel D3 receptor partial agonists and a potent D 3-selective antagonist in vivo for their effect in the cocaine-seeking behavior induced by reintroduction of cocaine-associated stimuli after a long period of abstinence, and without any further cocaine. Compound 5g, a nonselective partial D3 receptor agonist with a pharmacological profile similar to 3, and 5p, a potent and selective D 3 antagonist, reduced the number of active lever presses induced by reintroduction of cocaine-associated stimuli. However, 5q, a highly potent and selective D3 partial agonist, did not have any effect on cocaine-seeking behavior. Although brain uptake studies are needed to establish whether the compounds achieve brain concentrations comparable to those active in vitro on the D3 receptor, our experiments suggest that antagonism at D2 receptors might significantly contribute to the reduction of cocaine craving by partial D3 agonists.