1360119-00-1Relevant academic research and scientific papers
A Diarylpentanoid with Potential Activation of the p53 Pathway: Combination of in silico Screening Studies, Synthesis, and Biological Activity Evaluation
Moreira, Joana,Almeida, Joana,Loureiro, Joana B.,Ramos, Helena,Palmeira, Andreia,Pinto, Madalena M.,Saraiva, Lucília,Cidade, Honorina
, p. 2969 - 2981 (2021)
In silico studies of a library of diarylpentanoids led us to the identification of potential new MDM2/X ligands. The diarylpentanoids with the best docking scores obeying the druglikeness and ADMET prediction properties were subsequently synthesized and e
New MD2 inhibitors derived from curcumin with improved anti-inflammatory activity
Zhang, Yali,Liu, Zhiguo,Wu, Jianzhang,Bai, Bin,Chen, Hongjin,Xiao, Zhongxiang,Chen, Lingfeng,Zhao, Yunjie,Lum, Hazel,Wang, Yi,Zhang, Hong,Liang, Guang
, p. 291 - 305 (2018/02/21)
An overactive Toll-like receptor (TLR) signaling complex is a significant pathogenic factor of acute and chronic inflammatory diseases. The natural product curcumin is reported to inhibit the TLR4 co-receptor, MD2 (myeloid differentiation protein 2), but
Synthesis and evaluation of curcumin-related compounds for anticancer activity
Wei, Xingchuan,Du, Zhi-Yun,Zheng, Xi,Cui, Xiao-Xing,Conney, Allan H.,Zhang, Kun
experimental part, p. 235 - 245 (2012/08/28)
Sixty-one curcumin-related compounds were synthesized and evaluated for their anticancer activity toward cultured prostate cancer PC-3 cells, pancreas cancer Panc-1 cells and colon cancer HT-29 cells. Inhibitory effects of these compounds on the growth of PC-3, Panc-1 and HT-29 cells were determined by the MTT assay. Compounds E10, F10, FN1 and FN2 exhibited exceptionally potent inhibitory effects on the growth of cultured PC-3, Panc-1 and HT-29 cells. The IC50 for these compounds was lower than 1 μM in all three cell lines. E10 was 72-, 46- and 117-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. F10 was 69-, 34- and 72-fold more active than curcumin for inhibiting the growth of PC-3, Panc-1 and HT-29 cells, respectively. FN1 and FN2 had about the same inhibitory effect as E10 and F10 toward Panc-1 cells but were less active than E10 and F10 toward PC-3 and HT-29 cells. The active compounds were potent stimulators of apoptosis. The present study indicates that E10, F10, FN1 and FN2 may have useful anticancer activity.
CURCUMIN ANALOGS AND METHODS OF USE THEREOF
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Page/Page column 20; 25-26, (2012/03/09)
Curcumin analogs and methods of use thereof are provided.
