119378-70-0Relevant academic research and scientific papers
Design and synthesis of piperazine acetate podophyllotoxin ester derivatives targeting tubulin depolymerization as new anticancer agents
Sun, Wen-Xue,Ji, Ya-Jing,Wan, Yun,Han, Hong-Wei,Lin, Hong-Yan,Lu, Gui-Hua,Qi, Jin-Liang,Wang, Xiao-Ming,Yang, Yong-Hua
, p. 4066 - 4074 (2017/08/22)
In this paper, a series of podophyllotoxin piperazine acetate ester derivatives were synthesized and investigated due to their antiproliferation activity on different human cancer cell lines. Among the congeners, C5 manifested prominent cytotoxicity towar
Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: Binding characterization at D2/D3 receptors and elucidation of a pharmacophore model
Brown, Dennis A.,Kharkar, Prashant S.,Parrington, Ingrid,Reith, Maarten E. A.,Dutta, Aloke K.
supporting information; experimental part, p. 7806 - 7819 (2009/12/07)
A series of structurally constrained analogues based on hybrid compounds containing octahydrobenzo[g or f]quinoline moieties were designed, synthesized, and characterized for their binding to dopamine D2 and D3 receptors expressed in HEK-293 cells. Among the newly developed constrained molecules, trans-octahydrobenzo[f]quinolin-7-ol (8) exhibited the highest affinity for D2 and D3 receptors, the (-)-isomer being the eutomer. Interestingly, this hybrid constrained version 8 showed significant affinity over the corresponding nonhybrid version 1 (representing a constrained version of the aminotetralin structure only) when assayed under same conditions (Ki of 49.1 and 14.9 nM for 8 vs 380 and 96.0 nM for 1 at D2 and D3, respectively). Similar results were found with other lead hybrid compounds, indicating a contribution of the piperazine moiety in the observed enhanced affinity. On the basis of the data of new lead constrained derivatives and other lead hybrid derivatives developed by us, a unique pharmacophore model was proposed consisting of three pharmacophoric centers, two with aromatic/hydrophobic and one with cationic features.
Oxadiazole and thiadiazole derivatives of dihydropyridine NPY antagonists
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, (2008/06/13)
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I. wherein B is with X being O, S or and X1 is O or S. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
