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Chengdu, China

Wang S.,Shenyang Pharmaceutical University | Yan J.,Drug Screening Center | Wang X.,Shenyang Pharmaceutical University | Yang Z.,Shenyang Pharmaceutical University | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2010

In the course of studies directed toward the discovery of novel non-sugar α-glucosidase inhibitors for the treatment of diabetes, a series of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives was synthesized and evaluated as α-glucosidase inhibitors. Most compounds showed good inhibitory activity with IC50 values ranging from 0.0645 μM to 26.746 μM. 7-Hydroxy-6-methoxy-3-[4-(4-methylphenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one 7u manifested the most potent inhibitory activity with an IC50 value of 0.0645 μM. © 2009 Elsevier Masson SAS. All rights reserved.

Qian S.,Xihua University | Wu Y.,University of Sichuan | He Y.-X.,Xihua University | Wang Z.-Y.,Xihua University | And 2 more authors.
Gaodeng Xuexiao Huaxue Xuebao/Chemical Journal of Chinese Universities | Year: 2012

Some oleanolic acid(OA) derivatives with γ-lactone functionality in ring C had better H 2O solubi-lity and bioavailability than OA. Preliminary biological screening in vitro of these derivatives for 12 responding protein targets and cells of frequent diseases was processed. This investigation revealed that lactone 13 showed significant activity(IC 50=3.58 μg/mL) against Cathepsin K, and was found to be a potent leader compound for the treatment of osteoporosis. Preliminary structure-activity relationship analysis indicated that the γ-lactone and glyco-groups were active groups.

Wang S.,Shenyang Pharmaceutical University | Yan J.,Drug Screening Center | Wang J.,Shenyang Pharmaceutical University | Chen J.,Shenyang Pharmaceutical University | And 3 more authors.
European Journal of Medicinal Chemistry | Year: 2010

A number of 5-phenylisoxazole-3-carboxylic acid derivatives (5a-e, 11a-e) were synthesized and analyzed for their ability to inhibit xanthine oxidase. Most of the compounds exhibited potency levels in the micromolar/submicromolar range. The presence of a cyano group at the 3-position of phenyl moiety turned out to be the preferred substitution pattern, as its transformation into the nitro group determined a general reduction of the inhibitory potency. A molecular modeling study on compound 11a was performed to gain an insight into its binding mode with xanthine oxidase, and to provide the basis for further structure-guided design of new non-purine xanthine oxidase inhibitors related with 5-phenylisoxazole-3-carboxylic acid scaffold. © 2010 Elsevier Masson SAS. All rights reserved.

Qian S.,Xihua University | Qian S.,University of Sichuan | Li H.,University of Sichuan | Chen Y.,Drug Screening Center | And 3 more authors.
Journal of Natural Products | Year: 2010

Protein tyrosine phosphatase 1B (PTP1B) is a negative regulator in the process of insulin signaling and a promising drug target for diabetes and obesity. Derivatives of oleanolic acid were synthesized and evaluated as PTP1B inhibitors. Several derivatives exhibited moderate to good inhibitory activities against PTP1B, with 25f displaying the most promising inhibition (IC 50 = 3.12 μM). Structure-activity relationship analyses of these derivatives demonstrated that the integrity of the A ring and 12-ene moieties was important in the retention of PTP1B enzyme inhibitory activities. In addition, hydrophilic and acidic groups as well as the distance between the oleanene and acid moieties were associated with PTP1B inhibitory activities. Possible binding modes of 25f were explored by molecular docking simulations. © 2010 The American Chemical Society and American Society of Pharmacognosy.

Li J.,University of Sichuan | Pei S.,University of Sichuan | Zhu Y.,University of Sichuan | Wu J.,University of Sichuan | And 3 more authors.
Letters in Drug Design and Discovery | Year: 2012

A series of novel cis-furoquinoline derivatives was synthesized and tested for their antitumor activities in vitro against HepG2 cells, Lu-04 cells and Leu02 cells to evaluate structure-activity relationships. Assay-based antiproliferative activity study revealed that several compounds had significant effects on cytotoxicity, among which compounds 2f, 2l, 2q were found to be the most active compounds. Above all, compounds 2f, 2l, 2q would be potential anticancer agents which deserved further research. © 2012 Bentham Science Publishers.

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