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Shanghai, China

SHANGHAI HOTMED science CO. | Date: 2013-03-12

Disclosed in the present invention is a pharmaceutical composition, comprising a weight ratio of 1:120 to 1:1000 of camptothecin compound of formula I and -cyclodextrin or derivatives thereof, and an acidic buffer to adjust the pH=3.5-6.0. The composition can be used to treat solid tumours, such as melanoma, pancreatic cancer, hepatoma etc. The pharmaceutical composition of the present invention is miscible with a water-miscible co-solvent system in any proportion, and can be used as an intravenous infusion solvent, and has no obvious hemolysis or vascular stimulation; the pharmaceutical composition has a better tumour inhibiting rate than solubilisation of surfactants.

Ji H.,Northwestern University | Ji H.,University of Utah | Jing Q.,Northwestern University | Jing Q.,Shanghai Hotmed science Co. | And 2 more authors.
Tetrahedron | Year: 2012

2-Aminopyridinomethyl pyrrolidines represent a class of highly potent and selective neuronal nitric oxide synthase inhibitors. Conditions for a Mitsunobu reaction of a naphthol and a hindered secondary alcohol were optimized to give good to excellent yields. A key step in the synthesis of these inhibitors is the deprotection of the benzyl group from the N-Boc and N-Bn double protected 2-aminopyridine ring at a late stage of the synthesis, which has been proven difficult in our previous syntheses. Acetic acid was found to facilitate the N-Bn deprotection. © 2011 Elsevier Ltd. All rights reserved. Source

Tang K.,East China Normal University | Tang K.,Shanghai Hotmed science Co. | Huang J.,Shanghai Hotmed science Co. | Pan J.,Shanghai Hotmed science Co. | And 2 more authors.
RSC Advances | Year: 2015

Celastrol is a natural triterpenoid which possesses diverse pharmacological activities including potent antitumor activity. Previously, we reported a C(6)-modified celastrol derivative NST001A which possesses cytotoxic activity against Colon 205 cells with a 60 nM IC50 value. To further explore the structure activity relationships, a new class of C(6)-indole substituted celastrol derivatives were designed and synthesized. Biological evaluation of these compounds includes their cytotoxic activity against human hepatocellular carcinoma Bel7402 and human glioblastoma cell line H4. Among all these semisynthetic analogues, compound 4f and 4h displayed excellent in vitro antiproliferative activities against Bel7402 cancer cells (IC50 = 0.02 μM and 0.01 μM, respectively). This journal is © The Royal Society of Chemistry. Source

Tang K.,East China Normal University | Tang K.,Shanghai Hotmed science Co. | Huang Q.,East China Normal University | Zeng J.,Shanghai Hotmed science Co. | And 4 more authors.
Molecules | Year: 2014

New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer. Source

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