140486-19-7Relevant academic research and scientific papers
Modified norcantharidins: Synthesis, protein phosphatases 1 and 2A inhibition, and anticancer activity
Hart, Matthew E.,Chamberlin, A. Richard,Walkom, Cecilia,Sakoff, Jennette A.,McCluskey, Adam
, p. 1969 - 1973 (2004)
Fourteen modified norcantharidin analogues have been synthesised and screened for their ability to inhibit the serine/threonine protein phosphatases 1 and 2A. The most potent compounds found were 10 (PP1 IC50= 13±5 μM; PP2A IC50=7±3 μM) and 16 (PP1 IC 50=18±8 μM; PP2A IC50=3.2±0.4 μM). Overall, only analogues possessing at least one acidic residue at the former anhydride warhead displayed any PP1 or PP2A inhibitory action. The ability of these analogues to inhibit PP1 and PP2A correlates well with their observed anti-cancer activity against a panel of five cancer cell lines: A2780 (human ovarian carcinoma), G401 (human kidney carcinoma), HT29 (human colorectal carcinoma), H460 (human lung carcinoma) and L1210 (murine leukemia).
Camptothecin-glycine-norcantharidin conjugate and application thereof
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, (2019/12/29)
The invention provides a camptothecin-glycine-norcantharidin conjugate I and a preparation method thereof. R in the formula I is selected from C1-C6 alkyl groups, substituted alkyl groups, cycloalkylgroups, benzyl groups or substituted benzyl groups. Activity tests prove that the designed and synthesized camptothecin-glycine-norcantharidin conjugate I has an excellent antitumor effect, and especially has high activity on liver cancer, stomach cancer, colon cancer and pancreatic cancer. Additionally, the preparation method of the camptothecin-glycine-norcantharidin conjugate I has the advantages of easily available raw materials, low cost, high yield of the target product, and easiness in preparation.
Natural drug composition modified derivative and anti-tumor application thereof
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, (2019/04/17)
The invention discloses a camptothecin derivative I and a synthesis method thereof in the field of new drug design and synthesis. The structural formula of the camptothecin derivative I is as shown inthe specification, R in the formula I is selected from H, Br or dehydrogenation, and R1 is selected from C1-C3 alkyl, naphthenic base, benzyl and substituted benzyl. Activity tests prove that the designed and synthesized camptothecin derivative I has excellent anti-tumor effects and particularly is high in liver cancer, stomach cancer, colon cancer and pancreatic cancer activity.
Aromatic pyrrolidine amide prolyl endopeptidase inhibitors
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, (2008/06/13)
A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.
