docosahexaenoate has been researched along with Neoplasms* in 2 studies
2 other study(ies) available for docosahexaenoate and Neoplasms
| Article | Year |
|---|---|
Synthesis of new alkylaminooxysterols with potent cell differentiating activities: identification of leads for the treatment of cancer and neurodegenerative diseases.
We describe here the syntheses and the biological properties of new alkylaminooxysterols. Compounds were synthesized through the trans-diaxial aminolysis of 5,6-alpha-epoxysterols with various natural amines including histamine, putrescine, spermidine, or spermine. The regioselective synthesis of these 16 new 5alpha-hydroxyl-6beta-aminoalkylsterols is presented. Compounds were first screened for dendrite outgrowth and cytotoxicity in vitro, and two leads were selected and further characterized. 5alpha-Hydroxy-6beta-[2-(1H-imidazol-4-yl)ethylamino]cholestan-3beta-ol, called dendrogenin A, induced growth control, differentiation, and the death of tumor cell lines representative of various cancers including metastatic melanoma and breast cancer. 5alpha-Hydroxy-6beta-[3-(4-aminobutylamino)propylamino]cholest-7-en-3beta-ol, called dendrogenin B, induced neurite outgrowth on various cell lines, neuronal differentiation in pluripotent cells, and survival of normal neurones at nanomolar concentrations. In summary, we report that two new alkylaminooxysterols, dendrogenin A and dendrogenin B, are the first members of a class of compounds that induce cell differentiation at nanomolar concentrations and represent promising new leads for the treatment of cancer or neurodegenerative diseases. Topics: Amines; Animals; Cell Differentiation; Cell Line, Tumor; Cell Survival; Cholestanols; Dendrites; Drug Discovery; Humans; Mice; Neoplasms; Neurodegenerative Diseases; Spermidine; Stereoisomerism; Sterols | 2009 |
Synthesis and antitumor activity evaluations of albumin-binding prodrugs of CC-1065 analog.
An albumin-binding prodrug of the extremely potent CC-1065 analog, (+)-FDI-CBI, has been synthesized. This analog, (+)-FDI-CBIM, formed an albumin conjugate when added to human albumin in vitro. A greater amount (>3-fold) of the prodrug can be administered to animals compared to the free drug. The prodrug had significantly improved antitumor efficacy compared to the free drug in animal models using syngeneic animal tumors and human ovarian xenografted tumor cells. Antitumor drug delivery by in situ formation of drug-albumin conjugate is a promising strategy to improve antitumor efficacy. Topics: Animals; Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Disease Models, Animal; Duocarmycins; Female; Humans; Indoles; Mice; Molecular Structure; Neoplasm Transplantation; Neoplasms; Prodrugs; Serum Albumin; Structure-Activity Relationship | 2008 |