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Xia A.-B.,Zhejiang University of Technology | Wu C.,Zhejiang University of Technology | Xu D.-Q.,Zhejiang University of Technology | Wang Y.-F.,Zhejiang University of Technology | And 3 more authors.
Journal of Organic Chemistry | Year: 2013

The organocatalytic Michael reaction of ketones with γ- monohalonitrodienes catalyzed by chiral prolinethiol ether under solvent-free conditions was developed. The described method represents a novel approach for accessing highly functionalized monohaloalkenes with α, β-stereocenters of up to >99% ee. © 2013 American Chemical Society.


Li Z.-B.,Hangzhou Minsheng Pharmaceutical Group Co. | Shen L.-L.,Zhejiang University of Technology | Li J.-J.,Hangzhou Radio and University
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

The title compound, C7H7NO2S, adopts an E conformation about the C=C bond. The torsion angle C=C - C - C is -177.7 (3)°. The crystal structure features weak intermolecular by C - H⋯O interactions.


Zhang S.-J.,Zhejiang University of Technology | Ge Q.-F.,Hangzhou Minsheng Pharmaceutical Group Co. | Guo D.-W.,Hangzhou Minsheng Pharmaceutical Group Co. | Hu W.-X.,Zhejiang University of Technology | Liu H.-Z.,Zhejiang University of Technology
Bioorganic and Medicinal Chemistry Letters | Year: 2010

α-Lipoic acid derivatives were synthesized and evaluated for their in vitro anticancer activities against NCI-460, HO-8910, KB, BEL-7402, and PC-3 cell lines. The results, for most compounds exhibited dose-dependent inhibitory property and several compounds had good inhibitions at the dose of 100 μg/mL. Compound 17m was further selected for in vivo evaluation against S180 xenograft in ICR mice, which had 24.7% tumor-weight inhibition through intragastric administration of 200 mg/kg of body weight. Moreover, the LD50 in mice for 17m through ig exceeded 1000 mg/kg of body weight. © 2010 Elsevier Ltd. All rights reserved.


Zhang S.-J.,Zhejiang Chinese Medical University | Ding Z.-S.,Zhejiang Chinese Medical University | Jiang F.-S.,Zhejiang Chinese Medical University | Ge Q.-F.,Hangzhou Minsheng Pharmaceutical Group Co. | And 3 more authors.
MedChemComm | Year: 2014

A series of xanthone analogues modified from vadimezan 6 with carboxyl substitution were synthesized as esters, amides, arylidene hydrazides, diacylhydrazides and acyl thiosemicarbazides, and their structures were confirmed by IR, 1H NMR, MS, HRMS or elemental analysis. The in vitro anticancer activities were evaluated by the MTT method. It was found that compounds 8f, 8g and 10e were effective against A549 with an IC50 at 10.8 μM, 9.4 μM and 11.5 μM respectively, and that 8e was effective against HL-60 with an IC50 at 4.6 μM. Compounds 8f-h showed a significant inhibitory effect on HUVEC growth and migration in vitro, among which 8h inhibited HUVEC growth with an IC50 at 6.4 μM and HUVEC migration by 67.6% and 89.7% at 2.5 μg mL-1 and 10 μg mL -1 respectively. More spectacularly, docking study indicated that compound 8h might target the ATP binding site of VEGFR2. In addition, compounds 8a, 8f-h exhibited moderate in vivo antitumor efficacy against the S180 xenograft in ICR mice by 22.4-29.6% tumor weight inhibition. © 2014 the Partner Organisations.


Shi H.-B.,Zhejiang University of Technology | Shi H.-B.,Zhejiang Pharmaceutical College | Zhang S.-J.,Zhejiang University of Technology | Ge Q.-F.,Hangzhou Minsheng Pharmaceutical Group Co. | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

Thirty-seven (E)-1-(4-methyl-2-arylaminothiazol-5-yl)-3-arylprop-2-en-1- ones were synthesized via Claisen-Schmidt condensation of 1-(4-methyl-2- (arylamino)thiazol-5-yl)ethanone with the corresponding arylaldehydes. All these thiazolyl-chalcones were characterized and evaluated by MTT assay on human cancer cell lines BGC-823, PC-3, NCI-H460, BEL-7402 in vitro. Compounds 5, 8, 26, 37 and 41 are effective against cancer cell lines with IC50s below 10 μM. The antitumor activity in ICR mice bearing sarcoma 180 tumors indicates compounds 10 and 41 have moderate in vivo activity with 22-25% tumor-weight inhibition. © 2010 Elsevier Ltd. All rights reserved.


Li Z.-B.,Hangzhou Minsheng Pharmaceutical Group Co. | Li Z.-B.,Zhejiang University of Technology | Shen L.-L.,Zhejiang University of Technology | Zheng J.-A.,Jiaxing Zhonghua Chemical Industry Co.
Acta Crystallographica Section E: Structure Reports Online | Year: 2012

The title compound, C10H11NO2, adopts an E conformation about the C=C bond. The C=C - C=C torsion angle is 32.5 (3)°. The crystal structure features weak intermolecular C - H⋯O interactions. © 2012 International Union of Crystallography.


Wang Y.-F.,Zhejiang University of Technology | Chen R.-X.,Zhejiang University of Technology | Wang K.,Zhejiang University of Technology | Zhang B.-B.,Zhejiang University of Technology | And 2 more authors.
Green Chemistry | Year: 2012

The chiral squaramide derivatives as hydrogen bonding catalyst for the Michael addition reactions of 1,3-dicarbonyl compounds to nitroolefins under solvent-free conditions was developed using a planetary ball mill. High yields, high enantioselectivities and shorter reaction times were achieved with low catalyst loading. © 2012 The Royal Society of Chemistry.


Wang Y.,Zhejiang University of Technology | Chen R.,Zhejiang University of Technology | Li Z.,Hangzhou Minsheng Pharmaceutical Group Co. | Xu D.,Zhejiang University of Technology
Acta Crystallographica Section E: Structure Reports Online | Year: 2012

The title compound, C 14H 14BrNO 5, has two chiral C atoms. The quaternary C atom in the oxolanone ring has an S configuration, while the adjacent tertiary C atom has an R configuration. The oxolanone ring adopts an envelope conformation, with the flap C atom lying 0.298(3) Å from the mean plane of the remaining four atoms. In the crystal, molecules are connected into chains along [010] via weak C-H···O hydrogen bonds.


Wang Y.,Zhejiang University of Technology | Wang K.,Zhejiang University of Technology | Li Z.,Hangzhou Minsheng Pharmaceutical Group Co. | Xu D.,Zhejiang University of Technology
Acta Crystallographica Section E: Structure Reports Online | Year: 2012

The title compoud, C 19H 18BrNO 5, was synthesized by an organocatalytic reaction. The aymmetric unit contains two independent mol-ecules, in each of which the carbon between the two carbonyl groups adopts an R configuration, while the adjacent C atom has an S configuration. The dihedral angle between the two benzene rings is different in the two mol-ecules [11.64 (3) and 58.96 (4)°].


Shen L.-L.,Zhejiang University of Technology | Li Z.-B.,Zhejiang University of Technology | Li Z.-B.,Hangzhou Minsheng Pharmaceutical Group Co. | Li J.-J.,Hangzhou Radio and Television University
Acta Crystallographica Section E: Structure Reports Online | Year: 2012

The title compound, C9H8N2O4, adopts an E conformation about the C=C bond. The CHphen-yl-Cphen-yl-CH-C(-NO2) torsion angle is-57.7 (3)°. The crystal structure features weak inter-molecular C-H⋯O inter-actions.

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