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Qin S.-N.,Key Laboratory of Structure Based Drug Design and Discovery | Lu W.-W.,Shenyang Pharmaceutical University | Lu W.-W.,General Hospital of Shenyang Military Command | Wang Q.,Key Laboratory of Structure Based Drug Design and Discovery | And 2 more authors.
Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities | Year: 2013

One novel compound 3, 5-dimethoxy phthalimide had been isolated from Lasiosphaera fenzlii Reich. The compound exhibited definite antioxidant activity. Meanwhile it was reported that many compounds with the skeleton of phthalimide displayed many bioactivities such as anti-angiogenesis, anti-inflammatory, immune regulation and anti-tumor and so on. On the comprehensive review of above evidences, a series of N-substituted-3, 5-dimethoxy phthalimide derivatives and N-substituted-3, 5-dihydroxy phthalimide derivatives were designed and synthesized. Those compounds were synthesized by the multi-step reaction, 3, 5-dimethoxybenzoic acid was used as a starting material, and sequentially generates the phthalic anhydride and phthalimide, then reacted with a series of halogenated hydrocarbons, and stripped of methyl to obtain the target compounds. Thirty-one new compounds were synthesized, and the structures were characterized by 1H NMR, 13C NMR and MS techniques. Their anti-tumor and anti-angiogenesis activities against A549 and HUVEC cell line in vitro were tested. Some compounds showed a certain activity.

Liu J.,Shenyang Pharmaceutical University | Zhang Y.,Shenyang Pharmaceutical University | Li Q.,Shenyang Pharmaceutical University | Zhuang Q.,Shenyang Pharmaceutical University | And 5 more authors.
Molecular Medicine Reports | Year: 2014

The aim of the present study was to establish an improved method for in vitro guinea pig airway smooth muscle (ASM) cell culture and to evaluate the effect of 2-(4-amino- 3-chloro-5-trifluomethyl-phenyl)-2-tert-butylamino-ethanol hydrochloride (SPFF), a novel β2-adrenoceptor agonist, on the release of intracellular calcium in cells. A procedure for the efficient isolation, culture, passage and characterization of the cells was described. Primary ASM cells of guinea pigs were cultured by modified tissue cultivation. The cells were identified by their morphological characteristics and immunocytochemistry. The relative inhibition of the release of intracellular calcium by drugs in the cells was measured by fluorometric quantification with fluorochrome Fura-2/AM. The results were as follows: a) The ASM cells of the guinea pigs were successfully cultured and subcultured by using our improved method and typical peak-valley characteristics were observed under the phase contrast microscope; b) data from immunocytochemical staining with specific α-smooth muscle actin (α-SMA) demonstrated that the cells were ASM cells; c) the growth characteristics and cell viability demonstrated that the cells were in good condition and were able to be applied in the follow-up studies; d) the inhibitory effect of SPFF on the release of intracellular calcium was concentration-dependent when compared with the control and e) the potential mechanisms of SPFF on the inhibition of intracellular calcium may be independent of the ryanodine receptor, but may be closely associated with the inositol 1,4,5-trisphosphate receptor.

Liu S.-J.,Shijiazhuang University | Cui L.-B.,Shijiazhuang University | Xu H.-L.,Key Laboratory of Structure Based Drug Design and Discovery | Xu H.-L.,Shenyang Pharmaceutical University | And 7 more authors.
Heterocycles | Year: 2013

A series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were designed, synthesized and evaluated as dual binding site acetylcholinesterase inhibitors. The target compounds exhibited promising inhibitory activity for AChE. The structure-activity relationships were discussed and their binding conformation and simultaneous interactions mode were further clarified by the molecular docking studies. © 2013 The Japan Institute of Heterocyclic Chemistry.

Sun R.,Key Laboratory of Structure Based Drug Design and Discovery | Sun R.,Shenyang Pharmaceutical University | Song J.,Key Laboratory of Structure Based Drug Design and Discovery | Song J.,Shenyang Pharmaceutical University | And 12 more authors.
Chinese Chemical Letters | Year: 2011

The estrogen receptor is a target for therapeutic agents for hormone replacement in menopausal women, osteoporosis, reproductive cancers such as breast cancer, uterine cancer and prostate cancer. 1,4-Dihydrothieno[3′, 2′:5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives were designed, synthesized and biological evaluated as potential estrogen receptor antagonists. © 2010 Chun Hu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

Wang X.,Key Laboratory of Structure Based Drug Design and Discovery | Wang X.,Shenyang Pharmaceutical University | Sun R.,Key Laboratory of Structure Based Drug Design and Discovery | Sun R.,Shenyang Pharmaceutical University | And 12 more authors.
Medicinal Chemistry | Year: 2014

Estrogen receptors (ERs) are members of a superfamily of ligand-modulated nuclear receptors, which have been associated with an increased risk of cardiovascular diseases and breast cancer. Based on molecular docking studies, 1,4-dihydrothieno[3',2':5,6]thiopyrano[4,3-c]pyrazole-3-carboxamide derivatives as estrogen receptor inhibitors with a new scaffold, have been synthesized and tested for the antitumor activity on the ER expressing (ER dependent) human MCF-7 breast cancer cell line. According to the biological activity evaluation, compound 6a demonstrated the most potent antiproliferative activity (relative inhibitory rate: 100%). Several of these compounds exhibited moderate antitumor activity and worthy of further modification to obtain more potent anticancer candidate drugs. © 2014 Bentham Science Publishers.

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