115122-59-3Relevant articles and documents
Anhydride modified cantharidin analogues: Synthesis, inhibition of protein phosphatases 1 and 2A and anticancer activity
McCluskey, Adam,Bowyer, Michael C.,Collins, Elizabeth,Sim, Alistair T.R.,Sakoff, Jennette A.,Baldwin, Monique L.
, p. 1687 - 1690 (2000)
Two series of anhydride modified cantharidin analogues were synthesised and screened for their phosphatase inhibition (PP1 and PP2A) and cytotoxicity in various cancer cell lines (Ovarian A2780, ADDP; Osteosarcoma 143B; and Colon HCT116 and HT29). One series was synthesised by a novel, high yielding one-pot hydrogenation-ring-opening-esterification procedure, the other by acid catalysed acetal formation. Analogues 5-7 and 9 displayed moderate PP2A selectivity (ca. 5- to 20-fold) and inhibition typically in the low μM range (comparable, in some cases to cantharidin). The anticancer activity of these analogues varied with the cell line under study; however, many of them showed selective cytotoxicity for the colon tumour cell lines. (C) 2000 Elsevier Science Ltd. All rights reserved.
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.
