53261-25-9Relevant academic research and scientific papers
High-activity Pt complex as well as preparation method and application thereof
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Paragraph 0013, (2021/09/22)
The invention discloses a high-activity Pt (IV) complex, and belongs to the technical field of anticancer chemical drugs. The complex is represented by the general formula (1) or the general formula (2). General formula (1) (2) The invention introduces 6 - chloro -3 - methylbenzofuran -2 - formic acid or 5 -chloro -3 - methylbenzofuran -2 - formic acid into the platinum (IV) complex to significantly enhance the cytotoxicity of the platinum (IV) complex to cancer cells.
Tetravalent veratric acid platinum as well as preparation method and application thereof
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Paragraph 0031-0033; 0035-0036; 0038-0039, (2021/06/21)
The invention belongs to the technical field of medicine, and particularly relates to tetravalent veratric acid platinum as well as a preparation method and application thereof, the structural formula of the tetravalent veratric acid platinum is shown in the specification, and the preparation method comprises the following steps: (1) synthesizing hydroxyl platinum; (2) synthesizing tetravalent platinum veratryl acid; and (3) purifying tetravalent platinum veratryl acid. The tetravalent veratric acid platinum provided by the invention belongs to a tetravalent platinum prodrug, is a novel efficient anti-tumor active compound, has a broad-spectrum anti-cancer effect, is small in killing effect on normal cells of a human body, is efficient and low in toxicity, has a relatively high medicinal value, and is simple in preparation method, low in cost and easy for industrial production.
Tetravalent platinum complex containing posaconazole Preparation method and application thereof
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Paragraph 0085-0087, (2021/09/21)
The invention provides a tetravalent platinum complex containing posaconazole, a preparation method and application thereof, and the structure is shown in the formula I. The tetravalent platinum complex has obvious proliferation inhibition effect on liver cancer HepG2, lung cancer A549, colon cancer HCT116, breast cancer MDA-MB - 231 and cis-platinum drug-resistant lung adenocarcinoma, and the antitumor activity of the partial compound is obviously better than that of cisplatin. In addition, the complex has a remarkable inhibitory activity on common pathogenic fungi, shows significant inhibitory activity on posaconazole drug-resistant candida albicans, and can be used as a new drug for anti-tumor and antifungal candidate drugs.
Photothermal Therapy via NIR II Light Irradiation Enhances DNA Damage and Endoplasmic Reticulum Stress for Efficient Chemotherapy
Kong, Qingduo,Wei, Dengshuai,Xie, Peng,Wang, Bin,Yu, Kunyi,Kang, Xiang,Wang, Yongjun
, (2021/05/21)
Ovarian cancer has the highest death rate in gynecologic tumors and the main therapy for patients with advanced is chemotherapy based on cisplatin. Additionally, hyperthermic intraperitoneal has been used in clinic to obtain better efficacy for patients. Hence, combined photothermal therapy with platinum drugs in a new delivery system might bring new hope for ovarian cancer. A reduction sensitive polymer encapsulating a Pt (IV) prodrug and a near infrared II (NIR II) photothermal agent IR1048 to form nanoparticles were reported to enhance the efficacy of ovarian cancer treatment. At the same time, endoplasmic reticulum stress indicates an imbalance in proteostasis which probably caused by extrinsic stress such as chemotherapy and the temperature changed. The efficacy of nanoparticles containing Pt (IV) and IR1048 under NIR II light might be caused via increased DNA damage and endoplasmic reticulum (ER) stress.
Tetravalent platinum anticancer complex based on cis-platinum derivative containing ursodic acid ligand and preparation method and application thereof
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Paragraph 0023; 0055; 0058, (2021/11/19)
The invention belongs to the field of pharmaceutical chemistry, and particularly relates to a tetravalent platinum anticancer complex based on cis-platinum-derived ursodic acid ligand and a preparation method and application thereof. Pt (IV) Complex containing the ursolic acid ligand disclosed by the invention adopts cisplatin as a basic mother nucleus, the ursolic acid derivative ligand is introduced at one end in the axial direction, Cl or - OH groups are introduced at the other end. The preparation of the series Pt (IV) complex is cheap and easily available, the method is simple and feasible, the operation is easy, and the method is suitable for large-scale production. In-vitro experiments show Pt (IV) complexes US-CIS-CL and US-CIS-OH show high anticancer activity, superior to cisplatin, and have good anticancer activity.
Human serum albumin loaded tetravalent platinum nanoparticles and preparation method thereof
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Paragraph 0048-0050, (2021/06/21)
The invention relates to human serum albumin loaded tetravalent platinum nanoparticles and a preparation method thereof, the nanoparticles are formed by self-assembly of albumin and a tetravalent platinum drug modified with double aliphatic chains, the structural formula of the tetravalent platinum drug is as shown in formula I or formula II, and n and m are respectively and independently selected from integers of 1-15. The nanoparticles can respond to the environment in tumor cells to release platinum drugs, therefore effectively reduce the system toxicity, overcome the drug resistance of the tumor cells, and have the advantage of enhancing the killing effect on the tumor cells.
Low-toxicity Pt complex and preparation method and application thereof
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Paragraph 0022, (2021/07/08)
The invention discloses a low-toxicity Pt complex, and belongs to the technical field of anticancer chemical drugs. The structure of the complex is as shown in a general formula (1) or a general formula (2), pterostilbene is introduced into the platinum (IV) complex, and the anti-tumor effect of the platinum complex is improved and the toxic and side effects of the platinum complex on normal cells are reduced by utilizing the anti-inflammatory and anti-oxidation double functions of the pterostilbene.
Tetravalent platinum complex containing artesunate as well as preparation method and application of tetravalent platinum complex
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Paragraph 0045; 0047; 0048, (2021/07/08)
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.
Immunogenicity and cytotoxicity of a platinum(iv) complex derived from capsaicin
Sun, Yuewen,Yin, Enmao,Tan, Yehong,Yang, Tao,Song, Dongfan,Jin, Suxing,Guo, Zijian,Wang, Xiaoyong
supporting information, p. 3516 - 3522 (2021/03/23)
Platinum-based anticancer drugs constitute the cornerstone of chemotherapy for various cancers. Although cytotoxic agents are considered to have immunosuppressive effects, increasing evidence suggests that some cytotoxic compounds can effectively stimulate the antitumor immune response by inducing a special type of apoptosis called immunogenic cell death (ICD). A platinum(iv) complex (DCP) modified with the derivative of synthetic capsaicin (nonivamide) was designed to elicit ICD. The complex exhibited high cytotoxicity against a panel of human cancer cell lines including pancreas (PANC-1), breast (MCF-7), and liver (HepG2) cancer cells, and osteosarcoma (MG-63) cells. In addition to causing DNA damage, DCP also triggered the translocation of calreticulin (CRT) as well as the release of ATP and HMGB1 protein in PANC-1 cells, thus manifesting an efficient ICD-inducing effect on cancer cells. Furthermore, the DCP-treated PANC-1 cell-conditioned culture medium promoted the release of IFN-γ and TNF-α to induce the immune response of human peripheral blood mononuclear cells, thereby increasing their cytotoxicity to cancer cells. Concurrently, the phagocytosis of PANC-1 cells by macrophages was also augmented by DCP. The results demonstrate that DCP is an effective inducer of ICD and a potential agent for chemoimmunotherapy of cancers.
The invention discloses an amphipathic conjugate anti-tumor nano drug and a preparation method thereof. Nano-assembly and application
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Paragraph 0072; 0073, (2021/11/17)
The anti-tumor prodrug comprises at least one of a cisplatin precursor, a carboplatin precursor and an oxaliplatin precursor. The amphipathic conjugate anti-tumor nano-drug is simple in chemical structure, can be assembled into a uniform nano structure in water, can greatly reduce the damage to normal cells by reducing cytotoxicity of an antitumor drug outside the tumor cells, and has EPR effect in vivo so as to promote blood circulation time in a human body. Compared with a small molecule anti-tumor drug, the conjugate can prolong the blood circulation time in the human body and has a passive targeting function, so that the enrichment of the conjugate in the tumor site is greatly improved.
