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He G.,Hefei Medical Engineering Pharmaceutical Co.
Chinese Journal of Organic Chemistry

According to the scaffold hopping, a series of N-aryl-salicylamide derivatives, which have fragments of tyrosine kinase inhibitors lapatinib and neratinib were designed and synthesized. Their structures were identified by IR, 1H NMR, 13C NMR and MS techniques. The target compounds were tested for cytotoxic activity against four cancer cell lines, including A549, MCF-7, SGC-7901, Bel-7402, by methyl thiazolyl tetrazolium (MTT) in vitro. All the compounds demonstrated certain antitumor abilities, and some of them were better than gefitinib. © 2013 Chinese Chemical Society & SIOC, CAS. Source

Hu M.,Anhui University | Ye W.,Hefei Medical Engineering Pharmaceutical Co. | Li J.,Anhui University | Zhou P.,Anhui University | And 2 more authors.
Anti-Cancer Drugs

The signal transducer and activator of transcription 3 (STAT3) is constitutively activated in certain cancer cells. Therefore, blocking the aberrant activity of STAT3 in tumor cells is a validated therapeutic strategy. To discover novel inhibitors of STAT3 activity, we report the salicylanilide derivatives as a new small molecule inhibitor of the STAT3 signaling pathway. The N-(3-chloro-4-fluorophenyl)-2-hydroxy-4-(3-(piperidin-1-yl)propoxy) benzamide potently inhibited the activation and transcriptional function of STAT3. These studies further validate STAT3 as a drug discovery target and provide evidence that pharmacological agents that can selectively reduce the phospho-STAT3 levels in human cancer cells result in tumor apoptosis and growth inhibition. © 2015 Wolters Kluwer Health, Inc. All rights reserved. Source

Hu M.,Anhui University | Ye W.,Anhui University | Li J.,Anhui University | Zhong G.,Anhui University | And 3 more authors.
Chemical Biology and Drug Design

Two series of novel salicylanilide were synthesized as potential epidermal growth factor receptor (EGFR) inhibitors. The enzyme inhibitory activity against EGFR of all compounds was carried out, and their antiproliferative activities against the A549 and A431 cell lines were also evaluated. Of the compounds studied, majority of them exhibited high antiproliferative activities compared with gefitinib; especially, 12a and 12b exhibited stronger inhibitory activity against EGFR with IC50 values of 10.4 ± 2.25 and 15.4 ± 2.33 nM, respectively, which were comparable to the positive control of gefitinib (IC50 = 12.1 ± 2.21 nM). Compound 12b also showed outstanding inhibitory activity against A431 and A549 cell lines with the IC50 values of 0.42 ± 0.43 μM and 0.57 ± 0.43 μM, which was better than the positive controls. In the molecular modeling study, compound 12b was bound into the active pocket of EGFR with two hydrogen bond and with minimum binding free energy ΔGb = -25.1125 kcal/mol. The result also suggested that compound 12b could bind the EGFR kinase well. © 2014 John Wiley & Sons A/S. Source

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