Synthesis And Activity Of Erlotinib Derivatives

Erlotinib is used for treating the non-small cell lung cancer(NSCLC) that after failure of chemotherapy in clinical, and the mechanism for selectively blocking the epidermal growth factor receptor(EGFR) tyrosine kinase and autophosphorylation. However, with erlotinib widely used in clinical appeared, adverse reactions and drug resistance appeared in succession which due to secondary mutations in the gene, so urgent need for more drug which have better clinical anti-cancer effect.In this work, several Erlotinib derivatives were designed and synthesized by etherification, nitrification, reduction, cyclization, chlorinated, substitution, using 3,4-Dihydroxy-benzoic acid ethyl ester as starting materials. The structures of terminational compounds were determined by 1H NMR, 13 C NMR, IR and HRMS. The antitumor activities of these Erlotinib derivatives were evaluated by an MTT assay. The results reveal that some of the title compounds exhibit potent anti-proliferative activities against selected tumor cells. Among these compounds E-5, E-6, E-8, E-9, E-10, E-15 and E-19 against A549 were closest to Erlotinib.In this paper, preliminary fluorescence spectra test of these Erlotinib derivatives were measured, we found that emission wavelengths of most of these derivatives are in the visible region, there are some potential application values.Three new coordination polymers 1–3 have been synthesized by reactions of the N-(5-Amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine(AMPPA) with the Cd(NO3)2·4H2O. With the introduction of the building blocks of H2 ipa and H3 btc featuring 1D chain, 2D layer and 3D network. In addition, the Cd(II) ion effectively enhance the luminescence of the ligand.