a group of 1,3-biarylhydrazide derivatives possessing a cox-2 azido pharmacophore at the para- position of the c-1 phenyl ring in conjunction with a n-3 phenyl or substituted-phenyl ring (4-f,4-cl,4-ome) were designed and synthesized based on nucleophilic substitution reaction. a molecular modelling study of these compounds showed that the designed molecules were well bound with the active site...

A group of 1,3-biarylhydrazide derivatives possessing a COX-2 azido pharmacophore at the Para- position of the C-1 phenyl ring in conjunction with a N-3 phenyl or substituted-phenyl ring (4-F,4-Cl,4-OMe) were designed and synthesized based on nucleophilic substitution reaction. A molecular modelling study of these compounds showed that the designed molecules were well bound with the active site...

The 1,2,3-triazole is a well-known biologically active pharmacophore constructed by the copper-catalyzed azide–alkyne cycloaddition. We herein reported synthesis of 4-amino-7-chloro-based [1,2,3]-triazole hybrids via Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition 4-azido-7-chloroquinoline with an alkyne derivative acetaminophen. compound was fully characterized Fourier-transform infrared (FT...

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

Cancer is considered as a challenging deathly disease and discovering or synthesis of new cytotoxic agents is a worldwide attempt. In this study, a group of recently synthesized chalcones, with the structure of 1,3-diarylprop-2-en-1-one having differesnt COX-1 and/or COX-2 selectivities, have been examined on human hepatocarcinoma (HepG2), lung carcinoma (A549), and breast adenocarcinoma (MCF-7...

Cancer is considered as a challenging deathly disease and discovering or synthesis of new cytotoxic agents is a worldwide attempt. In this study, a group of recently synthesized chalcones, with the structure of 1,3-diarylprop-2-en-1-one having differesnt COX-1 and/or COX-2 selectivities, have been examined on human hepatocarcinoma (HepG2), lung carcinoma (A549), and breast adenocarcinoma (MCF-7...

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

cancer is considered as a challenging deathly disease and discovering or synthesis of new cytotoxic agents is a worldwide attempt. in this study, a group of recently synthesized chalcones, with the structure of 1,3-diarylprop-2-en-1-one having differesnt cox-1 and/or cox-2 selectivities, have been examined on human hepatocarcinoma (hepg2), lung carcinoma (a549), and breast adenocarcinoma (mcf-7...

Metastatic human pancreatic cancer cells (the SW1990 line) that are resistant to the EGFR-targeting tyrosine kinase inhibitor drugs (TKI) erlotinib and gefitinib were treated with 1,3,4-O-Bu3ManNAc, a 'metabolic glycoengineering' drug candidate that increased sialylation by ∼2-fold. Consistent with genetic methods previously used to increase EGFR sialylation, this small molecule reduced EGF bin...

Cancer is considered as a challenging deathly disease and discovering or synthesis of new cytotoxic agents is a worldwide attempt. In this study, a group of recently synthesized chalcones, with the structure of 1,3-diarylprop-2-en-1-one having different COX-1 and/or COX-2 selectivities have been examined on human hepatocarcinoma (HepG2), lung carcinoma (A549), and breast adenocarcinoma (MCF-7) ...