244219-94-1Relevant articles and documents
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors
Yang, Wei,Li, Lixuan,Wang, Yulan,Wu, Xiaowei,Li, Tingting,Yang, Nan,Su, Mingbo,Sheng, Li,Zheng, Mingyue,Zang, Yi,Li, Jia,Liu, Hong
, p. 5881 - 5890 (2015/11/11)
The design, synthesis and biological evaluation of a series of isoquinoline-based hydroxamic acid compounds as novel HDACs inhibitors were reported herein. A detailed SAR study showed most of the compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10c against HDAC1, 3, 6 were 4.17 ± 0.11 nM, 4.00 ± 0.10 nM, 3.77 ± 0.07 nM, respectively. Most of the compounds showed great anti-proliferative activities against RPMI 8226, HCT 116 and Hep G2 cells. The IC50 values of compounds 10a-h against RPMI 8226 cancer cell proliferation were all below 1 μM. HCT 116 cell was sensitive to the compounds 10a, 10f-g and 18a with the IC50 values 0.3 μM. The active compounds 10a-d did not show inhibitory activity against hERG channel. All these evidence indicated these compounds had great potential as HDACs inhibitors for the further development.
Synthesis and antimalarial activity of 7-benzylamino-1-isoquinolinamines
Gutteridge, Clare E.,Hoffman, Marshall M.,Bhattacharjee, Apurba K.,Gerena, Lucia
, p. 633 - 637 (2008/09/17)
(Chemical Equation Presented) Computer modelling suggests that 7-benzylamino-1-isoquinolinamines should mediate antimalarial effects by a mechanism distinct from that employed by existing antimalarial drugs. A series of these compounds was prepared in sev
Amide derivatives and nociceptin antagonists
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, (2008/06/13)
The present invention relates to a compound of the formula [1′] wherein R2is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1′] as an active ingredient. The compound [1′] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1′] as a nociceptin antagonist or analgesic.