8 results about "Topotecan" patented technology

The application discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method thereof and application of the compound in preparation of an antitumor chemotherapy drug sensitizer, and first prepares the steroid-indole diketopiperazine alkaloid hybrid compound from a fungus Aspergillus sp. EGF15-0-3 rice culture medium. The compound is a new skeleton compound first discovered in nature. It is first discovered that the hybrid compound has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. It is first discovered that the hybrid compound has chemotherapy sensitization activity on a tumor chemotherapy drug topotecan TPT, which provides a drug source molecule and data support for development of a new natural antitumor combination inhibitor, and has important significance for development and utilization of marine Aspergillus sp. fungus resources.

The anti-cancer use of a camptothecin derivative which demonstrates a surprising resistance to the degrading effects of Human Serum Albumin ("HSA") in vivo is disclosed. Since HSA represents about half of serum protein in human blood, previous camptothecins generally worked poorly or not at all in vivo due to inactivation by HSA among other factors. Since NSS-01 is similar in mechanism of action to other camptothecins, and as demonstrated herein has both: (i) greater anti-tumor activity against various human cancers and (ii) less toxicity at therapeutic dosing - than topotecan and irinotecan; and without wishing to be bound by theory, NSS-01 demonstrated desirable antitumor activity against adenocarcinomas, it therefore should demonstrate desirable antitumor activity against other cancers that are susceptible to Topoisomerase I inhibitors.

This invention relates to the preparation of 10-trifluoromethoxycamptothecin compounds and their use in antitumor drugs. The structural formula of these compounds is shown below. In vitro cytotoxicity screening results show that 10-trifluoromethoxycamptothecin compounds possess broad-spectrum antitumor activity, exhibiting strong inhibitory activity against human hepatocellular carcinoma cells (HepG2), human non-small cell lung cancer cells (A549), human colon cancer cells (SW480), human cholangiocarcinoma cells (QBC939), human breast cancer cells (MCF-7), human pancreatic cancer cells (PANC-1), and human pancreatic cancer cells (BxPC-3). Compounds 10-trifluoromethoxycamptothecin I and 7-ethyl-10-trifluoromethoxycamptothecin II showed strong inhibitory effects against all seven tested tumor cell lines, with IC50 values ​​exceeding 100%. 50 The concentrations were 0.913–0.0661 μM and 4.932–0.0578 μM, respectively, both significantly superior to the control drug topotecan. Among them, compounds I and II exhibited the strongest inhibitory activity against the BxPC-3 cell line, with IC50 values ​​of [missing value]. 50 The values ​​were 0.0661±0.0065μM and 0.0578±0.0043μM, respectively. Therefore, 10-trifluoromethoxycamptothecin compounds hold promise for development into a novel antitumor drug.

This invention discloses a non-cationic polymer siRNA and chemical drug co-delivery system, comprising a non-cationic polymer and a complex of siRNA and drug loaded on the polymer; the complex is composed of a target siRNA and a corresponding drug; the non-cationic polymer contains several branches with aromatic rings, the aromatic rings being selected from one or more of 5- to 15-membered aromatic rings or 5- to 15-membered heteroaromatic rings; the drug is selected from one or more of gemcitabine, mitoxantrone, topotecan, beloteccan, irinotecan, doxorubicin, camptothecin, and derivatives of any of the above drugs. This invention enables the synergistic delivery of siRNA and chemical drugs, effectively overcoming the cytotoxicity problems caused by cationic delivery systems, and demonstrates promising application prospects in the field of modern drug delivery.

Disclosed are methods, compositions, and kits for treating pediatric cancers using hydroxyureamethyl acylfulvene (LP-184) or pharmaceutically acceptable salts / solvates thereof. The methods include monotherapy and combination regimens for pediatric sarcoma, medulloblastoma, glioma (including DIPG), hepatoblastoma, Wilms tumor, and related malignancies. Combination therapies include LP-184 with vincristine, topoisomerase I poisons (topotecan or irinotecan), PARP inhibitors (e.g., rucaparib), or spironolactone, yielding additive or greater-than-additive reductions in tumor growth or cell viability.

The present application relates to a kind of preparation of new indole camptothecin derivatives and its use in antitumor, the structure of the compound general formula is shown as follows.In vitro cytotoxic activity screening results show that new indole camptothecin derivatives have broad-spectrum antitumor activity, to human hepatoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human intrahepatic cholangiocarcinoma cell (RBE), human breast cancer cell (MCF-7), human pancreatic cancer cell (BxPC3), human bladder cancer cell (T24), human bladder cancer cell (umuc3) show strong inhibitory activity. Among them, the antitumor activity of compound D-18 is most outstanding, and shows strong inhibition to the 8 tumor cell lines measured, IC 50 The range is 0.2585-10.69 μM, significantly better than the control drug irinotecan, and comparable to topotecan activity. Therefore, indole camptothecin derivatives are expected to be developed into a new antitumor drug.

This invention relates to a novel *Bletilla striata* alkaloid boric acid compound, its preparation method, and its use in the preparation of antitumor drugs. The general chemical formula of this class of compounds is shown in structural formulas (I) and (II). In vitro antitumor activity screening results showed that compounds of formulas I and II possess broad-spectrum antitumor activity, exhibiting strong inhibitory activity against human liver cancer (HepG2), human pancreatic cancer (SW1990), human ovarian cancer (A2780), human breast cancer (MCF7), and human colon cancer (SW480) cell lines. Compounds N-3 and N-4 showed strong inhibitory effects against all five tested tumor cell lines, with IC50 values ​​exceeding 100%. 50 The values ​​were 0.26–0.89 μM and 0.22–0.91 μM, respectively; compounds N-1, N-3, and N-4 exhibited strong inhibitory effects on the human pancreatic cancer (SW1990) cell line, with IC50 values ​​of 0.26–0.89 μM and 0.22–0.91 μM, respectively. 50 The concentrations were 0.97, 0.45, and 0.63 μM, respectively, significantly superior to the control drug topotecan; simultaneously, compounds N-3 and N-4 also exhibited strong inhibitory effects on the human breast cancer (MCF7) cell line, with IC50 values ​​of 0.97, 0.45, and 0.63 μM. 50 The concentrations were 0.80 and 0.65 μM, respectively, significantly better than the control drug topotecan. Therefore, the new cypermethrin borate compound holds promise for development into a novel antitumor drug.

The present application relates to a kind of preparation of trifluoromethyl camptothecin compound and its use in antitumor drugs, the structural formula of the compound is shown as follows.In vitro cytotoxic activity screening results show that trifluoromethyl camptothecin compound has broad-spectrum antitumor activity, to human hepatocellular carcinoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human cholangiocarcinoma cell (QBC939), human breast cancer cell (MCF-7), human pancreatic cancer cell (PANC-1), human pancreatic cancer cell (BxPC-3) shows strong inhibitory activity.4 trifluoromethyl camptothecin compounds I, II, III, IV all show strong inhibition to the 7 tumor cell lines measured, IC 50 Value is 0.503-0.0112 μM, 4.8477-0.6516 μM, 1.825-0.0005 μM and 4.9043-0.4612 μM, all significantly better than control drug topotecan. Among them, the compound shows the strongest inhibitory activity to BxPC-3 cell line, IC 50 Value is in the range of 0.6516-0.0005 μM. Therefore, trifluoromethyl camptothecin compound is expected to be developed into a new antitumor drug.