16 results about "Chlorambucil" patented technology

This invention provides a chlorambucil NO donor prodrug having the structure shown in Formula (I) or a pharmaceutically acceptable salt thereof: Formula (I). It involves reacting chlorambucil with a dihaloalkane to obtain a halochlorambucil intermediate; reacting the halochlorambucil intermediate with silver nitrate to obtain the chlorambucil NO donor prodrug. This invention applies the chlorambucil NO donor prodrug to the preparation of drugs for treating tumors, such as melanoma, lymphoma, leukemia, or breast cancer. This nanosystem exhibits good NO release levels under light irradiation. Cellular experiments have demonstrated its good antitumor effect, providing a new strategy for multimodal combined antitumor therapy.

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a heicogenin derivative as well as a preparation method and application thereof. The invention particularly relates to a preparation method for introducing amino acid, chlorambucil benzoate and chlorambucil butyrate derivatives at C3-OH sites of a heicogenin mother nucleus structure and application of the derivatives in preparation of anti-tumor drugs. The structure of the heicogenin spliced amino acid, chlorambucil benzoate and chlorambucil benzoate derivative and the pharmaceutically acceptable salt thereof is shown as a general formula I, II or III. Pharmacological experiments prove that the heicogenin derivative disclosed by the invention has a relatively good anti-tumor effect on human breast cancer cell lines and relatively low toxicity on human normal gastric mucosa epithelial cells GES-1, so that the heicogenin derivative has the potential of being developed into clinical anti-cancer drugs. # imgabs0 #

The present invention belongs to the field of biomedicine, and specifically relates to a diagnostic and therapeutic integrated probe responsive to carboxylesterase, and a preparation method and application thereof. The present invention discloses a small molecule diagnostic and therapeutic probe represented by the following structural general formula. This small molecule diagnostic and therapeutic probe is obtained by reacting a near-infrared fluorescent dye, chlorambucil, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC), and 4-dimethylaminopyridine (DMAP) in an organic solvent. The present invention encapsulates the above small molecule diagnostic and therapeutic probe with poly(lactic acid-co-glycolic acid)-polyethylene glycol (PLGA-PEG) to obtain a nano diagnostic and therapeutic integrated probe. The fluorescence wavelength of the obtained nano diagnostic and therapeutic integrated probe is located in the near-infrared region, which can realize near-infrared fluorescence imaging diagnosis of tumors, and has combined therapeutic properties of chemotherapy, photodynamic therapy, and sonodynamic therapy, and can significantly kill tumor cells.

This invention discloses a class of enzyme-activated prodrug compounds having the following general structural formula I: This invention discloses a class of enzyme-sensitive chlorambucil analog prodrugs. These prodrugs exhibit high selectivity for hypoxic tumors and can be effectively activated within hypoxic tumor cells. Upon specific activation, the prodrug releases free chemotherapeutic drug chlorambucil, simultaneously releasing the photosensitizer cyanine dye, achieving an "OFF-ON" photosensitivity conversion, and generating a large number of reactive oxygen species, thus achieving the unification and synergy of photodynamic therapy and activatable chemotherapy.

The application provides imidazotetrazine compounds or pharmaceutically acceptable salts thereof, and a preparation method and application thereof, and belongs to the technical field of medicines. The imidazotetrazine compounds or pharmaceutically acceptable salts thereof are obtained by connecting valproic acid, chlorambucil and borneol to an imidazotetrazine group through an ester bond or an amide bond by using a splicing principle. The imidazotetrazine compounds or pharmaceutically acceptable salts thereof have better antitumor activity, and a new generation of powerful antitumor drugs can be developed.

The present invention discloses an application of a dehydrogenated short peptide in the controlled release of anti-tumor drugs, wherein the dehydrogenated short peptide is applied to load chlorambucil to form a dehydrogenated short peptide-loaded chlorambucil gel DHPN1-CLB, thereby realizing the control of the in vitro release of chlorambucil, improving the aggregation of chlorambucil in cells during in vitro release, strengthening the anti-leukemia cell proliferation effect, and inducing cell apoptosis by decreasing the mitochondrial membrane potential of leukemia cells. The results show that the cell uptake experiment shows that the dehydrogenated short peptide-loaded chlorambucil gel DHPN1-CLB has a larger amount of aggregation in cells and is easier to enter cells. DHPN 1 can increase the aggregation of chlorambucil in cells, thereby enhancing the anti-leukemia cell proliferation effect. The chlorambucil-dehydrogenated peptide nanosystem induces cell apoptosis by decreasing the mitochondrial membrane potential of leukemia cells, and is time- and dose-dependent.

The invention belongs to the field of nano-drug delivery systems, and particularly relates to a double-sensitive type co-loaded emodin and chlorambucil micelle as well as a preparation method and application thereof. The structural formula of the polymer is as follows: polyethylene glycol monomethyl ether, p-hydroxymethyl phenylboronic acid pinacol ester and emodin grafted dendritic polymer p (mPEG-co-HPBE-co-EMD) are designed and synthesized by taking polymethacrylate as a connecting unit, and the dendritic polymer p (mPEG-co-HPBE-co-EMD) is used for entrapment of chlorambucil. The co-drug-loaded polymeric micelle can be used for co-delivery of the emodin and the chlorambucil, improves the water solubility of drugs, has proper particle size and ROS / pH dual sensitivity, can realize targeted release of the emodin and the chlorambucil at tumor sites, and realizes collaborative treatment of chemotherapy and oxidation therapy. In the # imgabs0 # formula, n = 30-85, and x: y: z = 1: (2-5): (1-3).

The invention discloses an eudecane type sesquiterpene lactone TBB chlorambucil heterocomplex and application thereof, the derivative is a compound TBB-DJ, and the structural formula of the derivative is as shown in the formula TBB-DJ. Experimental results show that the compound TBB-DJ has a remarkable inhibition effect on proliferation activity and migration ability of liver cancer cells, and shows a unique anti-hepatocellular carcinoma effect of the compound TBB-DJ. Therefore, the compound TBB-DJ has an important application prospect in research and development of anti-hepatocellular carcinoma drugs.

The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutical preparations, and relates to a nano preparation for targeting glioblastoma, and preparation and application thereof, in particular to a nano preparation of chlorambucil-mycophenolic acid prodrugs for targeting glioblastoma, especially temozolomide drug-resistant glioblastoma, and preparation and application thereof. According to the invention, firstly, a chlorambucil-mycophenolic acid prodrug or a pharmaceutically acceptable salt thereof is constructed, and then on the basis, a prodrug co-assembled nano preparation capable of realizing synergistic delivery of three drugs, namely chlorambucil, mycophenolic acid and MHY1485, is constructed. Meanwhile, the prodrug co-assembled nano preparation is subjected to targeted modification, so that the prodrug co-assembled nano preparation is endowed with the capability of crossing a blood brain barrier. A targeting peptide modified nano-drug delivery system is constructed through a prodrug co-assembly technology, blood brain barrier crossing and accurate delivery of drugs to tumor sites are achieved, and the synergistic anti-tumor effect of a drug combination is remarkably improved.

This invention belongs to the field of nanomedicine delivery systems, specifically relating to a dual-sensitivity co-loaded emodin and chlorambucil micelles, their preparation method, and applications. The polymer structure is as follows: Using polymethacrylate as the linking unit, this invention designs and synthesizes a dendritic polymer p(mPEG-co-HPBE-co-EMD) grafted with polyethylene glycol monomethyl ether, p-hydroxymethylphenylboronic acid pinacol ester, and emodin, and uses it for encapsulating chlorambucil. This co-loaded polymer micelle can be used for the co-delivery of emodin and chlorambucil. This co-loaded micelle improves the water solubility of the drug, has a suitable particle size, and dual ROS / pH sensitivity, enabling targeted release of emodin and chlorambucil at tumor sites, achieving synergistic treatment with chemotherapy and oxidative therapy. In the formula, n = 30-85, x:y:z = 1:2-5:1-3.

The invention discloses an iron-based nano composite material and a preparation method and application thereof. The invention relates to an iron-based nano composite material which is obtained by taking an iron-based metal organic framework material as a carrier, loading a medicine 1, wrapping the surface of the iron-based metal organic framework material with polydopamine and combining with a medicine 2 through a borate bond, the iron-based metal organic framework material is MIL-88, the medicine 1 is beta-lapamoquinone, and the medicine 2 is chlorambucil. The preparation method comprises the following steps: S1, preparing MIL-88; s2, preparing MIL-88-beta-lap (MIL-88-beta-lap) S3, MIL-88-beta-lap (PDA) is prepared, and MIL-88-beta- S4, cb-BA is prepared; s5, MIL-88-beta-lap (PDA)-cb is prepared, and the PDA-cb is prepared; the iron-based nano composite material is used as a drug carrier to be applied to tumor treatment. According to the invention, combined treatment of ferroptosis, photo-thermal treatment and chemotherapy can be realized.

The present invention relates to the field of biomedicine technology, and discloses a DNA damage prodrug, nanoparticles, a preparation method and an application. The DNA damage prodrug CSP of the present invention is a photosensitizer pyropheophorbide a (PPa) and a DNA damage agent chlorambucil (Cb) as a simulated drug, bridged by a GSH-responsive disulfide bond. The nano drug of the present invention is prepared by a nanoprecipitation method using the DNA damage prodrug of the present invention and the PARP inhibitor Olaparib. The present invention can realize the GSH-triggered release of chlorambucil and Olaparib in a high GSH concentration tumor microenvironment, thereby enhancing DNA damage and DNA damage repair dysfunction, respectively, and promoting the effect of chemotherapy-photodynamic synergistic therapy for breast cancer.

Pharmaceutical compositions comprising oil as a vehicle, a suspending agent, and a surfactant are disclosed to be used in conjunction with active pharmaceutical ingredients which are water soluble or insoluble, or which are sensitive to water but insoluble in oil. Such active pharmaceutical ingredients may include temozolomide, lenalidomide, Oxaliplatin, Cisplatin, Carboplatin, 5-fluorouracil, irinotecan, topotecan, cyclophosphamide, doxorubicin, vincristine, vinblastine, Melphalan, Chlorambucil, Dacarbazine, Daunorubicin, Epirubicin, Mitoxantrone, Etoposide, Teniposide, Azacitidine, Cytarabine, Gemcitabine, vinoralbine, Pemetrexed, a derivative thereof, or a combination thereof. The pharmaceutical compositions may be administered as an oral suspension. Other embodiments are directed towards methods of using and methods of making such formulations.

The invention belongs to the field of biological medicines, and provides a preparation method and application of a stapled peptide and micromolecular antitumor drug covalent conjugate with high stability and strong antitumor activity. Traditional micromolecular antitumor drugs such as camptothecin, chlorambucil and the like have the problems of low water solubility, low bioavailability, poor stability, drug resistance and the like. The camptothecin or chlorambucil is covalently coupled with the stapled peptide through AEA, so that the water solubility of the small molecule medicine is remarkably improved, the anti-tumor onset time is remarkably shortened, and the long-lasting tumor cell proliferation inhibition capability is shown. Compared with linear peptide, the stability of the stapled peptide is remarkably improved, and a polypeptide drug coupling strategy based on the stapled peptide solves the problem of poor stability of polypeptide in a coupled drug on one hand, and provides a new thought for further development of classical anti-tumor drugs on the other hand.

The invention relates to application of chlorambucil in prevention and control and growth promotion of panax notoginseng diseases. It is found that chlorambucil has a good pseudo-ginseng rust rot fungus inhibiting effect and a good growth promoting effect on beneficial bacteria such as mortierella and trichoderma and can be used for promoting growth of pseudo-ginseng, and therefore chlorambucil can be widely applied to pseudo-ginseng disease control and growth promoting.

The invention discloses an endoplasmic reticulum-targeted rhodium (I) complex, a preparation method and an application thereof. The structural formula of the targeted rhodium (I) complex is shown in Formula I. The preparation method comprises the following steps: Step 1, preparing a ligand: amino isonitrile and chlorambucil are subjected to amidation reaction to obtain a ligand; Step 2, preparing the targeted rhodium (I) complex: the ligand obtained in Step 1 is reacted with phenyl isonitrile rhodium (I) complex to obtain the targeted rhodium (I) complex of Formula I; the targeted rhodium (I) complex is applied to preparing anticancer drugs and preparing type II ICD inducer drugs; the targeted rhodium (I) complex of the invention not only has excellent antitumor activity, but also can be used as a type II ICD inducer to induce ICD in tumor cells; the preparation process is simple, the conditions are mild, and large-scale production is possible, and the industrial and practical application potential is available; the targeted rhodium (I) complex has good biocompatibility and is conducive to clinical use.