110482-92-3Relevant articles and documents
Synthesis and anticancer effect of 3,4,5-n-alkyl-benzamides on colon carcinoma HCT- 116 cells
Chan, Jilly Octaria Tagore,Arsianti, Ade,Marcelia, Maurin,Wijoyo, Stevano Julio,Fadilah, Fadilah,Putrianingsih, Rista,Azizah, Norma Nur,Tanimoto, Hiroki,Kakiuchi, Kiyomi
, p. 1362 - 1367 (2018)
The natural phenolic gallic acid has demonstrated a significant inhibition of cell proliferation in a series of cancer cell lines, as well as induced apoptosis in HCT-116 colon cancer cells. This research aims to synthesize six compounds of 3,4,5-trihydroxy-N-alkyl-benzamide derivatives of gallic acid, and investigate its anticancer effect on colon carcinoma HCT-116 cells.Six compounds of 3,4,5-trihydroxy-N-alkyl-benzamide, namely 3,4,5-trihydroxy-N-methyl-benzamide (2); 3,4,5-trihydroxy-N-ethyl-benzamide (3); 3,4,5-trihydroxy-N-butyl-benzamide (4); 3,4,5-trihydroxy-N-sec-butyl-benzamide (5); 3,4,5-trihydroxy-N-tert-butyl-benzamide (6) and 3,4,5-trihydroxy-N-hexyl-benzamide (7), have been successfully synthesized by amidation of carboxyl group of gallic acid with six corresponding alkylamines, respectively. Furthermore, anticancer effect of these six synthesized derivatives on colon HCT-116 cells were examined by MTT assay. Data were analyzed by linear regression method to generate IC50 value. The results will be compared with gallic acid as an original compound and doxorubicine as a positive control.Amidation of gallic acid with six corresponding alkylamines gave desired -N-methyl-, -N-ethyl-, -N-butyl-, -N-sec-butyl-, -N-ters-butyl-, and –N-hexyl benzamide with yield ranging from 18% to 84%. Compared to gallic acid (IC50: 0.05 μM) and doxorubicine (IC50: 0.001 μM), all these six synthesized derivatives showed a lower anticancer effect on colon HCT-116 cells. The strongest anticancer and inhibitory effect on HCT-116 cells has shown by 3,4,5-trihydroxy-N-hexyl benzamide (7) with IC50 value of 0.07 μM. Our results suggested that 3,4,5-trihydroxy-N-hexyl benzamide (7) is a potential to be developed as a promising anti-colon cancer agent.
HALOGENATED BENZOTROPOLONES AS ATG4B INHIBITORS
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Page/Page column 32; 38, (2018/06/12)
The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
Discovery of small-molecule inhibitors of the TLR1/TLR2 complex
Cheng, Kui,Wang, Xiaohui,Zhang, Shuting,Yin, Hang
, p. 12246 - 12249 (2013/02/23)
An important regulator of innate immunity, the protein complex of Toll-like receptors 1 and 2 (TLR1/TLR2) provides an attractive target for the treatment of various immune disorders. The novel compound CU-CPT22 can compete with the binding of the specific lipoprotein ligand to TLR1/TLR2 (see picture) with high inhibitory activity and specificity. Repression of downstream signaling from TNF-α and IL-1β was also observed. Copyright
