摘要：Accurate detection of multiple small end-metabolic biomarkers is more sensitive than large biomoleculesto provide real-time feedbacks of physiological/pathologicalstate, but is more challenging due to lack of specific identifyinggroups. Current optical platforms suffer from unsatisfactoryresolutions to differentiate each target because they producesimilar output to different targets using a single excitation,and inevitably involve non-functional components that increase chances of interacting with non-target ***, by taking full advantage of each building unit’sfunctionality to integrate multivariate recognition elements inone interface, a dual-excitation-driven full-component-responsive metal-organic framework (MOF)-based luminescentprobe, namely CeTMA-TMA-Eu, is successfully custom-tailored for detecting both pseudouridine (Ψ) and N-acetylaspartate (NAA), the diagnostic hallmarks of cancer andneurodegenerative disorder. Remarkably, Ψ interacts withMOF’s organic building unit (trimesic acid, TMA) and filtersout its absorptions of 262 nm-light to reduce its energytransferred to Eu^(3+), while NAA induces the valence transitionof Ce^(4+)/Ce^(3+) nodes to improve the cooperative energy transferefficacy from TMA and Ce^(3+) to Eu^(3+). As a result, this platformexhibits completely reverse photoresponses towards Ψ(“switch-off” at 262 nm excitation) and NAA (“switch-on”upon 296 nm excitation), and demonstrates excellent selectivity and sensitivity in complex biofluids, with low detection limits of 0.16 and 0.15 μM, and wide linear ranges of0–180 and 0–100 μM, respectively. Such full-componentresponsive probe with dual-excitation-mediated reverse responses for multi-small targets intrinsically minimizes its interaction with non-target molecules and amplifies resolutionto discriminate each target, providing a new strategy for improving assay accuracy of multi-small biomarkers in diagnostics.

摘要：Influenza A virus is the major cause of seasonal or pandemic flu worldwide. Two main treatment strategies vaccination and small molecule anti-influenza drugs are currently available. As an effective vaccine usually takes at least 6 months to develop, anti-influenza small molecule drugs are more effective for the first line of protection against the virus during an epidemic outbreak, especially in the early stage. Two major classes of anti-influenza drugs currently available are admantane-based M2 protein Mockers (amantadine and rimantadine) and neuraminidase (NA) inhibitors (oseltamivir, zanamivir, and peramivir). However, the continuous evolvement of influenza A virus and the rapid emergence of resistance to current drugs, particularly to amantadine, rimantadine, and oseltamivir, have raised an urgent need for developing new anti -influenza drugs against resistant forms of influenza A virus. In this review, we first give a brief introduction of the molecular mechanisms behind resistance, and then discuss new strategies in small-molecule drug development to overcome influenza A virus resistance targeting mutant M2 proteins and neuraminidases, and other viral proteins not associated with current drugs. (c) 2015 Chinese Pharmaceutical Association and Institute of Materia Medics, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

摘要：Several novel fluorescent probes targeting α_1-adrenergic receptors were well designed and synthesized by conjugating phenylpiperazine pharmacophore with coumarin and fluorescein fluorophores. These compounds showed suitable fluorescence property, high receptor affinity, and low cytotoxicity. Moreover, the cell imaging results displayed that these probes can be effective tools for the real-time detection of ligand-receptor interactions, as well as the visualization and location of α_1-adrenergic receptors in living cells.

摘要：By integrating photoinduced electron transfer（PET） into the design of functional bioluminogenic probes,Urano and his coworkers recently developed a new rational design strategy, BioLeT. It is expected that this BioLeT strategy will enable us to design and develop new bioluminescence probes for detecting various biomolecules with no catalytic or reactive activity.

摘要：Diamides acting on insect ryanodine receptors are an intensive research area now. In order to search for novel candidates, a series of diamides containing biphenyl substructure were designed and *** insecticidal activities against armyworms（Mythimna sepatara） and aphis（Aphis craccivora） were screened. The compounds with 3,5-dichloro-4-（1,1,2,2-tetrafluoroethoxy）phenyl substituent were found to be insecticidal to armyworms with the similar symptoms to poisoning by flubendiamide. In this research, we presented a novel type of diamide insecticide as a lead compound for further optimization.

摘要：Spiro heterocycles frequently occur in bioactive molecules. In the pursuit of neonicotinoids with spiro hererocycles, three types of novel neonicotinoids with spirobenzofuranone, spirooxindole or spiroacenaphythylenone framework were designed and synthesized. Insecticidal evaluation showed that some of spirobenzofuranone containing neonicotinoids exhibited moderate activity against cowpea aphid, armyworm or brown planthopper.

摘要：In this review, we retrospect our progress in biological active naphthalimide and analogues as antitumor agents in the past 20 years. On one hand, various derivations in naphthalimide pharmacophores were developed to enhance their DNA binding affinity and antitumor property thereby. Heterocyclic fused naphthalimides, bis-naphthalimides, non-fused substituted naphthalimides and the carboxamide derivatives were synthesized. For example, thio-heterocyclic fused-naphthalimides were designed and evaluated in comparison with their oxo-heterocyclic fused analogues. Extended or created heterocyclebased skeleton were also developed as antitumor agents. On the other hand, we broaden the design strategy of naphthalimide antitumor agents besides DNA intercalation and topo II poison. We have introduced more drug design methods, such as prodrugs, multitarget drugs, computer-aided drug design,photodynamic therapy. For example, we have got naphthalimide derivatives which inhibited topo II and induced LMP by introducing long alkyl chain and polyamines. Several representative compounds were clarified of their antitumor mechanism of action. In all, our research improves the structure diversity of naphthalimide antitumor agents and distinct variances of antitumor targets and mechanism of action.

摘要：A convenient and scalable synthesis of 1-amino-5-cyanonaphthalene was described.

摘要：Five multinuclear cyclotriphosphazene ligands were synthesized and tested for their cleavage activities to plasmid DNA. All of these new compounds were confirmed by MS, ^1H NMR, ^31P NMR, ^13C NMR and IR. Preliminary studies on the cleavage of pUC19 DNA in the presence of metal complexes were performed. The results revealed that these complexes could act as powerful catalysts under physiological conditions. The complexes 3b ＋ Cu can effectively cleave DNA to nicked form, giving hydrolysis rate constant of 0.08/h under physiological conditions. An acid-base catalyzed DNA phosphate-diester hydrolysis mechanism was also orooosed.

摘要：This paper presents a series of first- and second-generation click-modified coumarin-based fluorescent probes for thiols. These molecules demonstrate high turn-on fluorescent response and good selectivity towards aromatic thiols over other relevant reac- tive sulfur species, reactive oxygen species and common nucleophiles. Moreover, probe la can detect thiols in the reduced rabbit plasma sample. Therefore, this approach provides a particularly impressive tool for detecting thiol in biological systems.