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Design, synthesis and biological evaluation of novel arylidine-malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B
Springer Science and Business Media LLC - - 2013
Girdhar Singh Deora, Chandrabose Karthikeyan, N. S. Hari Narayana Moorthy, Vandana Rathore, Arun K. Rawat, Akhilesh K. Tamrakar, A. K. Srivastava, Piyush Trivedi
In this study, we describe the design, synthesis, biological evaluation and molecular modelling studies of novel non-carboxylic arylidine malononitrile-based molecules as Protein Tyrosine Phosphatase 1B (PTP1B) inhibitors. The synthesized derivatives were evaluated in vitro for glucose reuptake using L6 muscle cell lines and enzymatic assay against PTP1B. The biological activity results showed tha...... hiện toàn bộ
Pharmacophore modeling and 3D-QSAR studies of leucettines as potent Dyrk2 inhibitors
Springer Science and Business Media LLC - - 2014
Anu Bahl, Prashant Joshi, Sandip B. Bharate, Harish Kumar Chopra
Novel potential nonsedating H1 antagonists related to the gauche rotamer of PROS-NH-histamine
Springer Science and Business Media LLC - - 2009
R. M. Shafik, F. S. G. Soliman, Mona M. El‐Semary, M. N. S. Saudi, Rasha Y. Elbayaa
ECV304/C6 coculture model of the BBB coupled with LC–MS analysis for drug screening from Rhubarb extract
Springer Science and Business Media LLC - Tập 25 - Trang 1935-1944 - 2016
Jiang-Feng Yuan, Hui-Hui Ji, Zhi-Jun Qiu, Da-Hong Wang
The nature of blood–brain barrier permeation of most herbal medicines is unknown. To screen blood–brain barrier drug candidates from natural product library, an ECV304/C6 coculture model was established. The permeability parameters and morphological analysis showed that the cultured ECV304 cell monolayer was of integrity and vitality. A library of widely used medicinal plant rhubarb extract was sc...... hiện toàn bộ
In vitro production of reactive oxygen species (ROS) by sampangine
Springer Science and Business Media LLC - Tập 26 Số 6 - Trang 1170-1175 - 2017
Nasiri, Hamid R., Hohmann, Katharina, Hatemler, Melissa G., Plodek, Alois, Bracher, Franz, Schwalbe, Harald
Sampangine is an azaoxoaporphine alkaloid with interesting biological activities. Elucidating the mode of action of sampangine is a topic of continuous research. Recently reported cell-based data have indicated heme-dysfunction and subsequent reactive oxygen species production as being responsible for the biological activity of the natural product. By using an in vitro biochemical assay the abilit...... hiện toàn bộ
In vitro antiproliferative activity of 11-aminoalkylamino-substituted 5H-indolo[2,3-b]quinolines; improving activity of neocryptolepines by installation of ester substituent
Springer Science and Business Media LLC - Tập 22 - Trang 4492-4504 - 2013
Wen-Jie Lu, Marta Świtalska, Li Wang, Mizuki Yonezawa, Ibrahim El-Tantawy El-Sayed, Joanna Wietrzyk, Tsutomu Inokuchi
The research article describes the effect of an ester group on the in vitro antiproliferative activity in SAR studies of 5-methyl-5H-indolo[2,3-b]quinoline (neocryptolepine) derivatives. The C-2 and/or C-9 ester-substituted neocryptolepines were synthesized starting from indole-3-carboxylates and N-methylanilines, which were bearing an ester group. To these ester-substituted neocryptolepines, vari...... hiện toàn bộ
Modification and biological evaluation of novel 4-hydroxy-pyrone derivatives as non-peptidic HIV-1 protease inhibitors
Springer Science and Business Media LLC - Tập 20 - Trang 200-209 - 2010
Meizi He, Ning Yang, Chunlai Sun, Xiaojian Yao, Ming Yang
In this study, we have modified 4-hydroxy-pyran-2-ones, especially introduced heteroatoms (S or O) into the substituents, and detected their interactions with the binding pockets of HIV-1 protease (PR). The results indicated that the ethoxyl groups at C-2′ and C-5′ of the phenyl ring could enhance the affinities to the S 1 ′ and S ...... hiện toàn bộ
N, N’-disubstitutedphenyl-4-ethoxyl benzene-1, 3-disulfonamides: design, synthesis, and evaluation of anti-platelet aggregation activity
Springer Science and Business Media LLC - Tập 28 - Trang 1388-1401 - 2019
Xin Chen, Xiujie Liu, kai Qiu, Xiang Xu, Caiwen Li, Yan Wang
According to the bio-isosterism theory, a series of N, N’-disubstitutedphenyl-4-ethoxylbenzene-1, 3-disulfonamides (5a-p) were designed and synthesized by two steps of reactions including chlorosulfonation and ammonolysis. The structures of all compounds have been confirmed by IR, 1H-NMR, 13C-NMR, and ESI-MS spectra. The in vitro anti-platelet aggregation activities were evaluated by Born’s test i...... hiện toàn bộ
Synthesis, characterization & anticonvulsant activity of amide derivatives of 4-amino-1,2-naphthoquinone
Springer Science and Business Media LLC - - 2013
Mukesh Bansal, Bharat Goel, Shubhanjali Shukla, Radhey Shyam Srivastava
In the present study, 4-amino-1,2-naphthoquinone analogues were synthesized and characterized by spectroscopic (FT-IR, 1H NMR and 13C NMR) and elemental analysis. The synthesized compounds were evaluated for anticonvulsant activity by the maximal electroshock (MES) test and subcutaneous pentylenetetrazole (sc. PTZ) test, the most widely employed seizure models for early identification of anticonvu...... hiện toàn bộ
Ligand-based 3D-QSAR analysis and virtual screening in exploration of new scaffolds as Plasmodium falciparum glutathione reductase inhibitors
Springer Science and Business Media LLC - Tập 23 - Trang 25-33 - 2013
P. Kamaria, N. Kawathekar
Plasmodium falciparum glutathione reductases involved in redox homeostasis pathway of parasite are found to be the most emerging target in the treatment of malaria. In the present study, a 3D-QSAR pharmacophore model was developed, based on twenty-three 1,4-naphthoquinone derivatives reported previously with marked inhibition against glutathione reductase (GR). The pharmac...... hiện toàn bộ
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