98results about How to "Significant in vitro antitumor activity" patented technology

The invention discloses a new 1-azabenzanthrone-platinum (II) complex, i.e., monochloro.mono(dimethyl sulfoxide).mono(1-azabenzanthrone) platinum (II), as well as a synthesis method and an application thereof. The complex is prepared through the following steps: weighing equivalent amounts of 1-azabenzanthrone and dichloro-di(dimethyl sulfoxide) platinum (II); dissolving in a polar solvent; heating or performing reflux reaction to obtain a target product, wherein the synthesis can specifically be performed through a solution method or a solvothermal method. Investigation shows that the complex has anti-proliferative activity on human tumor cell strains such as HepG2, SK-OV-3, SK-OV-3 / DDP, BEL-7404, T-24 and HL-7702; the result shows that the complex has obvious in-vitro anti-tumor activity, has higher potential medicinal value and is expected to be used for preparing various anti-tumor medicaments. The chemical structural formula of the complex is shown in the specification.

The invention discloses synthesis of a 9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex targeted to liver cancer and an application of the complex and belongs to the technical field of medicines. The invention aims to provide a dichloro-dimethyl-sulfoxide-9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex having a novel structure, and a synthesis method and an application thereof.The chemical structure formula of the dichloro-dimethyl-sulfoxide-9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex is represented as follow. The complex can be used for producing antitumor medicines.

The invention belongs to the field of medicinal chemistry and discloses pyrimidotriazole compounds containing hydrazine bonds as well as a preparation method and an application of the pyrimidotriazole compounds in drug preparation. The general formula I of the compounds is shown in the specification. The compounds have remarkable inhibition and killing functions on multiple tumor cells such as MGC-803, MCF-7 and EC-109, can serve as candidate or lead compounds for further development and are applied to preparation of an anti-tumor drug.

The invention discloses a new platinum (II) complex of 6-amino oxoisoaporphine, namely monochloro.dimethyl sulfoxide.6-amino oxoisoaporphine platinum (II), and a synthesis method and an application thereof. The complex is synthesized by the steps of dissolving 6-amino oxoisoaporphine and dichloro.di(dimethyl sulfoxide) platinum (II) in a polar solvent, and heating or carrying out a reflux reaction to obtain the target product; specifically the complex can be synthesized by a solution method, and can also be synthesized by a solvothermal method. Through investigation of proliferation inhibitory activity of the complex against HepG2, BEL-7404 and NCI-H460 and other human tumor cell strains, the complex is found to have significant in-vitro antitumor activity against the 3 kinds of tumor strains and have relatively good potential medicinal value, and is expected to be used in preparation of various antitumor medicines. The complex has the chemical structure represented by the following formula as described in the specification.

The invention discloses a 9-amino oxidized isoaporphine-platinum (II) complex, a synthetic method and an application thereof. The 9-amino oxidized isoaporphine-platinum (II) complex is prepared with 9-amino oxidized isoaporphine and dichloro bis(dimethyl sulfoxide)platinum (II) as raw materials through a coordination reaction in a polar solvent. A research result shows that the inhibition effect of the complex on telomerase reaches 56.97% and is improved significantly than those of a 1-aza-benzanthrone platinum (II) complex and 6-hydroxy oxidized isoaporphine-platinum (II) complex. The complex has significant inhibition effect on the activity of the telomerase and has excellent selectivity and significant in-vitro antitumor activity on various human tumor cell strains and a normal liver cell strain. The structure formula of the complex is represented as the formula (I).

The invention discloses a platinum (II) complex, a synthetic method and an application of the platinum (II) complex. The platinum (II) complex takes 4'-(4-N,N-diethylamine phenyl)-2,2':6', 2''-terpyridyl as a ligand. The complex is obtained by dissolving a compound as shown in a formula (II) and dichloro.di(dimethyl sulfoxide)-platinum in a polar solvent and performing a complexing reaction; the complex can be synthesized through a solution method specifically, and can also be synthesized through a solvothermal method. An applicant investigates the proliferating inhibitory activity of the complex to multiple human tumor cell lines, and the results show that the complex has a remarkable antitumor activity in vitro, has good potential medicinal value and is expected to be used for the preparation of all kinds of antitumor drugs. The chemical structural formula of the complex provided by the invention is shown as the following formula (I).

The invention discloses a triazolyl-containing amino-dithio formic ether compound as well as a preparation method and application of the compound which is taken as a new antineoplastic medicament lead compound, belonging to the field of pharmaceutical chemistry. According to the invention, 1, 2, 3-triazole active fragment is introduced into the structure of amino-dithio formic ether by click chemistry, thus the preparation method is simple, efficient and environment-friendly. The triazolyl-containing amino-dithio formic ether compound has the structure general formula shown in the specification, and has excellent antineoplastic activity for multiple tumour cells, can be used as a candidate or lead compound for the further development to be applied to the preparation of the antineoplastic medicaments.

The invention discloses a copper metal complex and a compound prepared from the copper metal complex and human serum albumin as well as a synthesis method and application thereof. The synthesis method of the copper metal complex comprises the following steps: taking phenyl-2-pyridyl ketone and 4,4'-dimethyl-3-thiosemicarbazide, taking an alcohol material as a solvent, reacting, generating precipitate, collecting the precipitate and washing the precipitate to obtain a ligand; taking the ligand which is phenyl-2-pyridyl ketone and contracting 4,4'-dimethyl-3-thiosemicarbazide and CuC12.2H2O, taking the alcohol material as the solvent, reacting, enabling a reactant to stand, crystallizing and collecting crystals to prepare the copper metal complex. The compound is prepared by incubating the copper metal complex and human serum albumin through a solution process. The structure of the copper metal complex is as shown in the following formula (I) which is as shown in the description.

The invention discloses 2,4,6-trisubstituted pyrimidine compounds containing 1,2,3-triazole, a preparation method and application thereof in preparation of medicine and belongs to the field of medicinal chemistry. A pyrimidine parent nucleus and a 1,2,3-triazole activity unit are combined by using classical click chemistry to simply and efficiently synthesize the 2,4,6-trisubstituted pyrimidine compounds containing 1,2,3-triazole in an environment-friendly manner. The 2,4,6-trisubstituted pyrimidine compounds containing 1,2,3-triazole have a structure general formula as shown in the specification. In vitro anticancer activity tests show that the compounds have a certain inhibition effect on many tumor cells including EC-109, MCF-7, MGC-803 and B16 and can be applied to preparation of an antitumor medicine, as a further developed candidate or lead compound.

The invention discloses a novel platinum (II) coordination compound of an oxidation iso-aporphine alkaloid (namely mono-chloride-dimethylsulfoxide-6-hydroxide radical oxidation iso-aporphine platinum (II)) and a synthesizing method and application of the mono-chloride-dimethylsulfoxide-6-hydroxide radical oxidation iso-aporphine platinum (II). According to the coordination compound, 6-hydroxide radical oxidation iso-aporphine and dichloro-dimethylsulfoxide platinum (II) which are equal in amount of substance are weighed and dissolved in a polar solvent, and a target product is obtained after a heating reaction or a reflux reaction; in detail, a solution method can be used for synthesizing, and meanwhile a solvothermal method can be used for synthesizing. Proliferation inhibition, on HepG2, SK-OV-3, SK-OV-3 / DDP, BEL-7404, T-24 and other human tumor cell stains, of the coordination compound is investigated, the result shows that the novel platinum coordination compound has obvious anti-tumor activity in vitro and good potential medicinal value and is expected to be used for preparation of kinds of anti-tumor drugs. The chemical structural formula of the coordination compound is as follows (please find the formula in the specification).

The invention discloses a high-activity coumarin-platinum (II) complex targeting the ovarian cancer and a synthesis method and application thereof. The complex adopts a chemical structural formula shown as one of formulae 1-5. A coumarin derivative is modified by natural coumarin as a skeleton, and then reacts with metal platinum (II) to form a complex so as to obtain the coumarin platinum (II) complex with higher activity. The in-vitro antitumor activity of the complex is far higher than that of other classical cisplatin anticancer medicines, and the complex also shows in-vitro antitumor activity superior to that of a coumarin ligand; the complex has a potential medicinal value and is expected to be applied to preparation of various antitumor medicines.

The invention discloses an LSD1 (lysine specific histone demethylase 1) inhibitor with a trans-diaryl ethylene structure, as well as a preparation method and application thereof in preparation of an anti-tumour medicament, and belongs to the technical field of medicinal chemistry. The compound disclosed by the invention has a general formula which is as shown in the description; in-vitro LSD1 enzyme inhibiting activity and anti-tumour activity experiments prove that the compound has an obvious inhibiting effect on tumour cells by inhibiting the activity of LSD1, can serve as a lead compound for further development, and is applied to preparation of anti-tumour medicaments.

The invention discloses small molecule degradation agents targeting at androgen receptors, belongs to the field of biological medicines, and particularly relates to a series of compounds for degradingandrogen receptor proteins in a targeted ubiquitination manner, a synthesis method and medical applications of the compounds, in particular in prevention or treatment of androgen receptor related diseases. Meanwhile, a series of in-vitro anti-tumor activity evaluation tests are carried out on the synthesized compounds by invertors of the invention, and the compounds have certain inhibitory activity on cancer cells.

The invention discloses a series of new 6-hydroxyloxoisoaporphine rare earth complexes, having a structural general formula as shown in specification, wherein Ln is La, Ce, Pr, Nd, Sm, Eu, Gd, Tb or Dy. The complexes are synthesized from 6-hydroxyloxoisoaporphine and the rare earth metal nitrates (Ln(NO3)3.xH2O as raw materials through a heating or reflux reaction. According to the complexes and the synthetic method and application thereof disclosed by the invention, the proliferation inhibition activity of the complexes to a plurality of human tumor cell strains such as SK-OV-3, SK-OV-3 / DDP and T-24 is investigated, and results indicate that all of the complexes have remarkable antitumor activity in vitro; in particular, the 6-hydroxyloxoisoaporphine lanthanum complex has extremely remarkable activity to cervical cancer cells SK-OV-3; in addition, apart from the 6-hydroxyloxoisoaporphine europium complex, the other complexes all have a good inhibition effect on human ovarian cancer / cis-platinum persisters SK-OV-3 / DDP.

Novel targeting antineoplastic benzimidazole derivative platinum (II) and ruthenium (II) complexes are disclosed. The chemical structure of the platinum (II) complex is shown in the description. The chemical structure of the ruthenium (II) complex is shown in the description. The platinum (II) complex and the ruthenium (II) complex show excellent antitumor activity in vitro, and have potential medicine value. Preparation methods and applications of the two complexes are also provided.

The invention discloses a copper metal complex and a compound of copper metal complex and human serum albumin, as well as synthesis methods and application of the copper metal complex and the compound. The synthesis method for the copper metal complex comprises the following steps of reacting 2-di-pyridyl ketone with 4,4minute-dimethyl-3-thiosemicarbazide to generate precipitates by taking an alcohol substance as a solvent, and collecting and washing the precipitates to obtain ligands; reacting the ligands with CuCl2.2H2O by taking an alcohol substance as a solvent, standing and crystallizing a reaction product, and collecting crystals to obtain the copper metal complex. The compound is obtained by incubating the copper metal complex and the human serum albumin by adopting a solution method. The structure of the copper metal complex is shown in Formula (I).

The invention discloses a 5-bromo oxoisoaporphine, and a synthesis method and application thereof. The synthesis route of the 5-bromo oxoisoaporphine comprises the following steps: reducing 4-bromobenzylcyanide used as an initial raw material to obtain 4-bromobenzylethylamine, reacting the 4-bromobenzylethylamine with phthalic anhydride, and performing Friedel-Crafts acylation cyclization reaction twice, thus obtaining the 5-bromo oxoisoaporphine through synthesis. The applicant surveys the proliferation inhibition activity of the 5-bromo oxoisoaporphine on multiple human tumor cell strains, and results show that the 5-bromo oxoisoaporphine has remarkable in-vitro antitumor activity, has good potential pharmaceutical values and is hopefully used for the preparation of various antitumor medicaments. The chemical structural formula of the 5-bromo oxoisoaporphine is shown as below in the specification.

The invention discloses a 2-phenylpyridine dual-core palladium (II) complex. The structural formula of the complex can be seen in the description. The invention further discloses a preparing method ofthe 2-phenylpyridine dual-core palladium (II) complex. The method includes the steps of evenly mixing glacial acetic acid, palladium acetate and 2-phenylpyridine, conducting complete reaction under stirring and heating, conducting cooling to the room temperature, removing glacial acetic acid to obtain reddish brown liquid, adding a polarity solvent, and conducting standing until yellow crystals are separated out thoroughly to obtain the 2-phenylpyridine dual-core palladium (II) complex. The invention further discloses application of the 2-phenylpyridine dual-core palladium (II) complex. The 2-phenylpyridine dual-core palladium (II) complex has remarkable in-vitro antineoplastic activity and cytotoxicity selectivity and is simple in preparing method and easy to industrially produce.

The invention discloses a tetravalent platinum complex containing artesunate. The structure of the tetravalent platinum complex is shown as a general formula I or II, wherein R is shown in the specification, and R1 is a branched chain or straight chain saturated C1-C20 alkyl group, or a branched chain or straight chain unsaturated C1-C20 alkyl group. The tetravalent platinum complex containing artesunate provided by the invention has an obvious proliferation inhibition effect on liver cancer HepG2, lung cancer A549, intestinal cancer HCT116, breast cancer MDA-MB-231 and cis-platinum drug-resistant lung cancer, the anti-tumor activity of part of compounds is obviously superior to that of cis-platinum, and the tetravalent platinum complex containing artesunate can be used as anti-tumor candidate drugs for deeper research.

The invention discloses two novel ruthenium and rhodium metal complexes taking lysicamine as ligands as well as a synthetic method and application of the two novel ruthenium and rhodium metal complexes. The synthetic method of the ruthenium and rhodium metal complexes comprises the following steps: dissolving dichloro.tetra(dimethyl sulfoxide) ruthenium (II) or rhodium trichloride and lysicamine into a polar solvent, and performing complexation reaction to prepare the ruthenium and rhodium metal complexes, wherein the ruthenium and rhodium metal complexes can be synthesized by virtue of solution methods or solvothermal methods. After the applicants investigate the proliferation inhibition activity of the ruthenium and rhodium metal complexes on human tumor cell lines such as NCI-H460, HepG-2, DLD-1 and MGC80-3 and the toxicity of the ruthenium and rhodium metal complexes to human normal liver cells HL-7702, results show that the ruthenium and rhodium metal complexes have significant in-vitro anti-tumor activity, and the activity of a rhodium metal complex is equal to that of cis-platinum; moreover, the ruthenium and rhodium metal complexes have relatively low cytotoxicity to normal cells, have good potential medicinal values, and are expected to be applied to the preparation of various anti-tumor medicines; and structural formulas of the complexes are respectively shown in the following formula (I) and formula (II) in the specification.

The disclosed ERJT-12 as the derivative of water-soluble constituent of radix salvia miltiorrhiza is composed by natural 5-(3-hydroxypropyl)-7-methoxy-2-(3-methoxy-4- hydroxy)-3-benzo[b] furaldehyde. Wherein, this compound takes microtubule as target, has obvious growth inhibition to multiple human tumor cells, can block the MCF-7 cell on mitosis time, and restrains the polymerization of tubulin.

The invention discloses a platinum (II) complex by taking chiral 4-(2,3-dyhydroxylpropyl)-methanamide-6-aza-benzanthrone as a ligand as well as a synthetic method and application of the platinum (II) complex. The synthetic method of the complex comprises the following steps: dissolving (+)-4-(2,3-dyhydroxylpropyl)-methanamide-6-aza-benzanthrone or (-)-4-(2,3-dyhydroxylpropyl)-methanamide-6-aza-benzanthrone and dichloro.bi(dimethyl sulfoxide)mixed platinum (II) in a polar solvent, mixing to carry out a complexing reaction, thereby obtaining the platinum (II) complex. The complex obtained by the inventor has obvious in-vitro antitumor activity, the in-vitro antitumor activity of a tested tumor strain is universally higher than that of an original chiral ligand, and the complex has high potential medicinal value and is expected to be used for preparing various antitumor medicines. The structural formulas of the complex disclosed by the invention are respectively shown in the formulas (I) and (II) in the specification.

The invention discloses a preparation method of a cholic acid-naphthalimide anti-tumor lead compound, belongs to the field of chemical synthesis of medicaments, and particularly relates to a synthesis method of a new naphthalimide compound with a chemical structural general formula shown in the specification. The preparation method of the compound is economical, simple, mild and effective. The obtained compound has extremely high inhibitory activity on HepG2 cells; and compared with phase-II clinic lead compound methylamphetamine, the compound partially has more superior inhibitory activity and can be used for preparing anti-tumor medicaments.

The invention discloses a 9-benzothianthrene hydrazine-ruthenium (II) complex as well as a synthetic method and an application thereof. According to the complex, 9-benzothianthrene hydrazine and dichloro*tetra (dimethyl sulfoxide) ruthenium (II) are taken as raw materials and have a complexing reaction in a polar solvent, and a target product is prepared. Researches show that the complex has better selectivity and remarkable in-vitro antitumor activity on various human tumor cell lines including Hep-G2, MGC80-3, SK-OV-3, BEL-7402 and NCI-H460 tumor cells, has better potential pharmaceutical value and is expected to be applied to preparation of various antitumor drugs. The structural formula of the complex is represented as a formula (I) in the specification.

The invention discloses a ruthenium (II) complex using chiral 4-(2,3-dihydroxypropyl)-formamide-6-azabenzanthrone as a ligand as well as a synthesis method and an application of the Ruthenium (II) complex. The synthesis method of the complex comprises the following steps: dissolving (+)-4-(2,3-dihydroxypropyl)-formamide-6-azabenzanthrone or (-)-4-(2,3-dihydroxypropyl)-formamide-6-azabenzanthrone and dichloro-tetra(dimethyl sulfoxide) ruthenium (II) into a polar solvent, then mixing, and performing complexing reaction to obtain the complex. The applicant discovers that the obtained complex has significant in-vitro anti-tumor activity, the in-vitro anti-tumor activity of tested tumor strains is universally higher than that of the original chiral ligand, and the complex has good potential medicinal value and is expected to be applied to preparation of various anti-tumor medicaments. The structural formula of the complex is respectively shown in formula (I) and formula (II) in the specification.

The invention discloses an acetylpyrazine thiosemicarbazone metal chelating agent as well as a preparation method and application of a metal complex of the acetylpyrazine thiosemicarbazone metal chelating agent. The synthesis method of the acetylpyrazine thiosemicarbazone metal chelating agent comprises the following steps: with 2-acetylpyrazine and 4, 4-diethyl thiosemicarbazone as raw materialsand an alcohol substance and hydrochloric acid as solvents, carrying out a reaction to generate a yellow precipitate, collecting the precipitate, and washing the precipitate to obtain a ligand; takingthe obtained ligand and a metal salt, and carrying out a reaction with the alcohol substance and acetonitrile as solvents, carrying out standing treatment on the reactant, and separating out and collecting the crystal, so as to obtain the acetylpyrazine thiosemicarbazone metal chelating agent and the metal complex thereof. The acetylpyrazine thiosemicarbazone metal chelating agent and the metal complex thereof have remarkable anti-tumor activity and can be used for tumor treatment.

The invention provides a 6H-indolo[2,3-b]quinoxaline derivative, and a preparation method and application thereof. The general formula is as shown in the specification. The preparation method comprises a step of preparing the 6H-indolo[2,3-b]quinoxaline derivative by taking o-phenylenediamine, indoldione, dihaloalkane and amine compounds as raw materials. The compounds provided by the invention show good antitumor activity.

The invention discloses a preparation method of a monoterpenoid indole alkaloid compound with a novel chemical structure from ochrosia borbonica and a medical application of the compound in preparation of a targeted anti-tumor drug by employing protein tyrosine kinase as a target. The compound is a novel monoterpenoid indole alkaloid compound. The compound has significant anti-tumor activity, has protein tyrosine kinase-inhibition activity equivalent to a positive control drug, and has the prospect of being developed into the targeted anti-tumor drug by employing the protein tyrosine kinase as the target.

The invention discloses a ruthenium fluorescent probe, and a preparation method, application and an application product thereof. The structural formula of the ruthenium fluorescent probe is as shown in the specification. The preparation method comprises the following steps: enabling 2,6-diacetyl pyridine and 4-hydroxybenzhydrazide to react by taking an alcohol substance as a solvent, collecting the precipitate generated by the reaction, and washing to obtain a ligand 2,6-diacetyl pyridine condensed 4-hydroxybenzohydrazine; (2) enabling the ligand 2,6-diacetyl pyridine condensed 4-hydroxybenzohydrazine and RuCl3 to react by taking the alcohol substance as the solvent, and then, sanding the reacted solution for separating crystals, and collecting the crystals to obtain the ruthenium fluorescent probe. The ruthenium fluorescent probe is used for preparing an anti-tumour medicament or a tumour detecting agent to obtain the anti-tumour medicament or the tumour detecting agent. The rutheniumfluorescent probe has good potential medicinal value and detection value, and is expected to be used in the preparation of various anti-tumour medicaments or tumour detecting agents.

The invention discloses two new manganese and zinc metal complexes taking alocasia amazonica alkali as a ligand as well as a synthesis method and an application of the manganese and zinc metal complex. The manganese and zinc metal complexes are obtained by dissolving manganese perchlorate or zinc perchlorate and alocasia amazonica alkali in a polar solvent, and carrying out a complexing reaction; the manganese and zinc metal complexes specifically can be synthesised through a solution method or a solvothermal method. The applicant finds that the two new manganese and zinc metal complexes show up superior in-vitro anti-tumour activities compared with the alocasia amazonica alkali ligand by inspecting the proliferation inhibition activities of the two new manganese and zinc metal complexes on human tumour cell strains of NCl-H460, HepG-2, DLD-1, MGC80-3 and the like, and the toxicities of the two new manganese and zinc metal complexes on human normal hepatic cells HL-7702, wherein the zinc metal complex has a low toxicity on normal cells and a good potential medicinal value, and is expected to be used for preparing various anti-tumour medicines. The structural formulas of the complex are shown in formula (I) and formula (II) specified in the description.