In a new and environmentally sustainable approach, a series of 2-arylimidazo[1,2-a]pyridine derivatives were synthesized in aqueous media in the presence of iodine as a catalyst. The reaction proceeded by condensation of various aryl methyl ketones with 2-aminopyridines to afford 2-arylimidazo[1,2-a]pyridines in good overall yields. Although several of the reactions were efficiently performed "on water", the addition of a surfactant, namely, sodium dodecyl sulphate , was found effective in terms of substrate scope and yield enhancement. Both methods were successfully used for the gram-scale synthesis of a marketed drug, zolimidine. The simple experimental setup, water as "green" media, and inexpensive catalyst are some of the merits of this protocol.

Iodine Promoted Efficient Synthesis of 2-Arylimidazo[1,2-a]pyridines in Aqueous Media: A Comparative Study between Micellar Catalysis and an "On-Water" Platform.

Post-condensational modifications of the Groebke‐Blackburn‐Bienaymé reaction products for scaffold-oriented synthesis

A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity

Tissue factor-targeted antibody-drug conjugate

The invention discloses a method for building medicine transport models for research on BCRP (breast cancer resistance proteins) mediation for 3D (three-dimensional) organs of the small intestines of mice. The method includes separating crypts from the small intestines of the mice by means of digestion, suspending the crypts in matrigel and then joining the crypts with cell culture plates and promoting differentiation of the crypts by the aid of ADMEM/F12 media with Respondin-1, m-noggin and m-EGF cell differentiation growth factors to form the 3D organs; carrying out morphologic observation and detecting the expression level of BCRP genes and proteins to verify the feasibility of model theories; carrying out research on the trans-membrane transport activity of BCRP in the 3D organs by the aid of fluorescent substrates Hoechst 33342 of the BCRP and inhibitors Ko143 or YHO-13177 of the fluorescent substrates by co-incubation processes. The method has the advantages that the medicine trans-cell-membrane transport in-vitro models for the research on the BCRP mediation for the 3D organs of the small intestines of the mice are built for the first time, and the method for building the models is easy and convenient to implement and high in detection efficiency and speed and can be widely applied to screening BCRP substrates and inhibitors in an in-vitro manner.

Method for building BCRP (breast cancer resistance proteins) mediated medicine transport models for research on 3D (three-dimensional) organs of small intestines and application

Facile synthesis of new functionalized 3,4-dihydro-2H-pyrroles using 2-isocyanoacetates

ThThe invention provides a disubstituted maleic amide connexon coupled with an antibody as well as a preparation method and an application thereof, and concretely provides a new kind of connexon whichis used for coupling a substance with high cytotoxic activity and a biomacromolecule. The kind of connexon can be selectively effected on a disulfide chain, and substance homogeneity of a conjugate is substantially improved. A conjugate prepared by the connexon has high inhibitory activity for cell strains for expressing corresponding antigens. The invention also provides a preparation method andan application of the conjugate.

Disubstituted maleic amide connexon for coupling antibody and medicament as well as preparation method and application thereof

Facile Synthesis of New Functionalized Triazacyclopenta[cd]indenones Through a Multicomponent Reaction Followed by an Intramolecular Aminolysis

The invention discloses an antibody-drug conjugate Pertuzumab-MCC-DM1 (P-DM1) having a structure represented by a formula shown in the specification, and a therapeutic agent composition containing the P-DM1 and an HER2 dimerization inhibitor antibody. The therapeutic agent composition contains a therapeutically effective amount of the P-DM1 and a therapeutically effective amount of the HER2 dimerization inhibitor antibody. The invention also discloses a method for treating higher proliferation diseases of illnesses. The method is characterized in that the therapeutically effective amount of the P-DM1 and the therapeutically effective amount of the HER2 dimerization inhibitor antibody are applied to mammals or people needing like treatment. Pertuzumab is coupled with maytenin alkaloid DM1 to obtain the conjugate P-DM1, and the composition containing the conjugate P-DM1 and the HER2 dimerization inhibitor antibody has synergistic effects in cancer growth inhibition in vivo and in vitro in order to realize a good treatment effect on HER2 mediated illnesses, such as cancers.

Antibody-drug conjugate Pertuzumab-MCC-DM1, conjugate and Trastuzumab composition, and application of conjugate and composition

The invention provides a double-substituted maleic amide connexon coupled with an antibody as well as a preparation method and application of the connexon. Particularly, a strong cytotoxic activity substance and biological macromolecules are coupled through a kind of new connexon. The kind of connexon can selectively act with a disulfide chain at the same time, so that the substance homogeneity and stability of a conjugate are greatly improved. The conjugate prepared from the connexon has high inhibitory activity for cell strains which express corresponding antigens. The invention further provides a preparation method and application of the conjugate.

Double-substituted maleic amide connexon for antibody-medicine coupling as well as preparation method and application of connexon

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Di-substituted maleic amide linker for antibody-drug conjugating and preparation method and use thereof

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