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Luo C.,Shenyang Pharmaceutical University | Sun J.,Shenyang Pharmaceutical University | Sun J.,Tianjin Institute of Pharmaceutical Research | Sun B.,Shenyang Pharmaceutical University | He Z.,Shenyang Pharmaceutical University
Trends in Pharmacological Sciences | Year: 2014

Despite the rapid developments in nanotechnology and biomaterials, the efficient delivery of chemotherapeutic agents is still challenging. Prodrug-based nanoassemblies have many advantages as a potent platform for anticancer drug delivery, such as improved drug availability, high drug loading efficiency, resistance to recrystallization upon encapsulation, and spatially and temporally controllable drug release. In this review, we discuss prodrug-based nanocarriers for cancer therapy, including nanosystems based on polymer-drug conjugates, self-assembling small molecular weight prodrugs and prodrug-encapsulated nanoparticles (NPs). In addition, we discuss new trends in the field of prodrug-based nanoassemblies that enhance the delivery efficiency of anticancer drugs, with special emphasis on smart stimuli-triggered drug release, hybrid nanoassemblies, and combination drug therapy. © 2014 Elsevier B.V. All rights reserved.

Wang H.,Shandong University | Meng F.,Tianjin Institute of Pharmaceutical Research
Theoretical Chemistry Accounts | Year: 2010

Water-assisted proton-catalyzed hydrolytic deamination of adenine to produce hypoxanthine has been studied using density functional theory method. Because adenine could be protonated at N1, N3, N7 and N10, four pathways initiated from the four different protonated adenines have been investigated. The first step of the four pathways is the nucleophilic attack of water with an assistant water to form a tetrahedral structure complex, and this is the rate-determining step. Including solvent effects decreased the relative energies of stationary points but have little effect on the structures. Pathway A is preferred due to the lowest energy barrier, and the relative free energy is 28.9 kcal/mol in vacuo. The outcomes show that adenine deamination under acidic condition is much easier to occur than under neutral condition due to lower energy barriers. The total atomic charge of C5 in the initial intermediate is correlated with the ease of deamination reaction. The more positive C5 atom is, the easier the deamination reaction is. © 2010 Springer-Verlag.

Tianjin Institute of Pharmaceutical Research | Date: 2011-01-14

The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof, wherein, the definitions of R

Tianjin Institute of Pharmaceutical Research | Date: 2012-11-12

A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.

Tianjin Institute of Pharmaceutical Research | Date: 2013-12-05

The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R

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