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Norcantharidin and analogues: synthesis and biological …

Hepatocellular carcinoma (HCC) is the most commontype of liver cancer and is one of the leading causes of cancerdeaths worldwide. Because of the complex mechanisms of HCC,effective therapies toward HCC have not significantly improved(,). As a heterogeneous tumor, HCC involvesmultiple pathways and molecular alterations (). With medical technology advances,there are increasing number of new treatments towards HCC,including surgical resection, liver transplantation andchemotherapy or immuno-biological cancer therapy. Cantharidin,which is extracted from the Chinese blister beetle, has been usedfor many years in Chinese medicine to treat tumors. However,because of nephrotoxic and other side effects, norcantharidin(NCTD) was synthesized in an effort to reduce toxicity. Currently,NCTD is widely used in the treatment of tumors (,).

Title:Synthesis and Antiproliferative Assay of Norcantharidin Derivatives in Cancer Cells

Chen YJ, Tsai YM, Kuo CD, Ku KL, Shie HSand Liao HF: Norcantharidin is a small-molecule synthetic compoundwith anti-angiogenesis effect. Life Sci. 85:642–651. 2009. : :

Norcantharidin (NCTD) inhibits DNA synthesis in DU145 cells.

Norcantharidin (NCTD) is a Chinese FDA approved, chemically synthesized drug for cancer treatment

Hill TA, Stewart SG, Ackland SP, GilbertJ, Sauer B, Sakoff JA and McCluskey A: Norcantharimides, synthesisand anticancer activity: Synthesis of new norcantharidin analoguesand their anticancer evaluation. Bioorg Med Chem. 15:6126–6134.2007. : :

Chen YJ, Tsai YM, Kuo CD, Ku KL, Shie HSand Liao HF: Norcantharidin is a small-molecule synthetic compoundwith anti-angiogenesis effect. Life Sci. 85:642–651. 2009. : :

Synthesis of norcantharidin‐dimer derivatives, Journal …

New Norcantharidin Analogs: Synthesis and Anticancer Activity

Hill TA, Stewart SG, Sauer B, Gilbert J,Ackland SP, Sakoff JA and McCluskey A: Heterocyclic substitutedcantharidin and norcantharidin analogues-synthesis, proteinphosphatase (1 and 2A) inhibition, and anti-cancer activity. BioorgMed Chem Lett. 17:3392–3397. 2007. :

Hill TA, Stewart SG, Ackland SP, GilbertJ, Sauer B, Sakoff JA and McCluskey A: Norcantharimides, synthesisand anticancer activity: Synthesis of new norcantharidin analoguesand their anticancer evaluation. Bioorg Med Chem. 15:6126–6134.2007. : :

Synthesis of a norcantharidin-tethered guanosine: …
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Synthesis of Norcantharidin Derivative, …

Norcantharidin (NCTD) inhibits DNAsynthesis in DU145 cells. DU145 cells were treated with or without100 μM NCTD for 24 h. (A) Cells were incubated with BrdU for1 h following treatment with NCTD for 24 h. The BrdU-positive cellswere then identified by immunofluorescence staining and observedunder a fluorescence microscope. (B) The proportion ofBrdU-positive cells. Data are expressed as the means of thepercentage of BrdU-positive cells ± SD. *P

New Norcantharidin Analogs: Synthesis and Anticancer …

Norcantharidin (NCTD) inhibits DNAsynthesis in DU145 cells. DU145 cells were treated with or without100 μM NCTD for 24 h. (A) Cells were incubated with BrdU for1 h following treatment with NCTD for 24 h. The BrdU-positive cellswere then identified by immunofluorescence staining and observedunder a fluorescence microscope. (B) The proportion ofBrdU-positive cells. Data are expressed as the means of thepercentage of BrdU-positive cells ± SD. *P

Pharmaceutical & Medicinal Chemistry

Chen YJ, Tsai YM, Kuo CD, Ku KL, Shie HSand Liao HF: Norcantharidin is a small-molecule synthetic compoundwith anti-angiogenesis effect. Life Sci. 85:642–651. 2009. : :

Synthesis and anticancer activity of a ..

Second, furan (3) and maleimide (13) were heated in toluene to afford dihydroxynorcantharimide (14) by the Diels-Alder reaction. Hydrogenation was then performed as a reduction in dry THF in the presence of catalytic 10% Pd/C to give norcantharimide (15). The lipophilic substitution of these derivatives all took place at -position of norcantharimide. The compounds 6, 14 or 15 reacted with alkyl or terpenyl bromide in dry acetone in the presence of K2CO3 to produce -substituted derivatives 1624 in moderate to excellent overall yields, as shown in . Using compounds 2224 as precursors we obtained compounds 2527 in moderate to excellent yields through hydrogenation reactions. The synthetic reactions were also outlined in . The chemical structures of these compounds were elucidated by 1H-NMR, 13C-NMR, 2D NMR and LC-MS spectroscopic methods.

Norcantharidin solid | Sigma-Aldrich

The key starting material in this study was 5,6-dehydronorcantharidin (5), which was prepared on a large scale through -selective cycloaddition, or Diels-Alder reaction, of furan (3) and maleic anhydride (4). Subsequent hydrogenation of 5 (H2, 10% Pd/C) using a modified procedure of McChuskey [] provided the starting norcantharidin (2) in excellent yield, which then was employed as the substrate for the synthesis our designed derivatives. First, norcantharidin (2) was reacted with hydroxylamine hydrochloride in the presence of sodium methoxide in dry methanol at room temperature to produce -hydroxynorcantharimide (6), according to a previous report. -Hydroxynorcantharimide (6) was then reacted with terpenyl or alkyl bromide in dry acetone in the presence of K2CO3 to afford -substituted derivatives 712 in moderate to good yields, as shown in .

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