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A novel and efficient macrolactonization of ω-hydroxycarboxylic acids using 2-methyl-6-nitrobenzoic anhydride (MNBA)
A variety of lactones were prepared in high yields at room temperature from the corresponding ω-hydroxycarboxylic acids using 2-methyl-6-nitrobenzoic anhydride in the presence ofExpand
Search for novel anti-tumor agents from ridaifens using JFCR39, a panel of human cancer cell lines.
Results indicate that RIDs-SB1 and RID-SB8 are interesting candidates for novel anti-cancer agents with unique modes of action. Expand
Ridaifen-SB8, a novel tamoxifen derivative, induces apoptosis via reactive oxygen species-dependent signaling pathway.
It is concluded that RID-SB8 exerts an anticancer effect via a mode of action distinct from tamoxifen, and that RIDs could become a promising anticancer lead compound which selectively induces ROS formation and apoptosis in cancer cells. Expand
A New Condensation Reaction for the Synthesis of Carboxylic Esters from Nearly Equimolar Amounts of Carboxylic Acids and Alcohols Using 2-Methyl-6-nitrobenzoic Anhydride
Various carboxylic esters were obtained in excellent yields with high chemoselectivities from nearly equimolar amounts of carboxylic acids and alcohols using 2-methyl-6-nitrobenzoic anhydride withExpand
Induction of mitochondria‐involved apoptosis in estrogen receptor‐negative cells by a novel tamoxifen derivative, ridaifen‐B
The results suggest that the induction of apoptosis by ridaifen‐B, a novel tamoxifen derivative, is dependent on mitochondrial perturbation without estrogen receptor involvement. Expand
Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents.
It was discovered that 13 and 16 strongly inhibit the viability of the HL-60 human acute promyelocytic leukemia cell line, whereas 14 possesses a medium activity against the same cell line and 15 has no effect on the cell viability. Expand
M-COPA, a Golgi Disruptor, Inhibits Cell Surface Expression of MET Protein and Exhibits Antitumor Activity against MET-Addicted Gastric Cancers.
The results offer an initial preclinical proof of concept for the use of M-COPA as a candidate treatment option for MET-addicted GC, with broader implications for targeting the Golgi apparatus as a novel cancer therapeutic approach. Expand
Targeting the Golgi apparatus to overcome acquired resistance of non-small cell lung cancer cells to EGFR tyrosine kinase inhibitors
Results provide the first evidence that targeting the Golgi apparatus might be a promising therapeutic strategy to overcome the vicious cycle of TKI resistance in EGFR-mutated NSCLC cells via downregulating cell surface RTK expression. Expand
Family-wide Analysis of the Inhibition of Arf Guanine Nucleotide Exchange Factors with Small Molecules: Evidence of Unique Inhibitory Profiles.
The presence of the membrane-binding domain in Legionella RalF reveals a strong inhibitory effect of BFA that is not measured on its GEF domain alone, and this study demonstrates the value of family-wide assays with incorporation of membranes to enable accurate dissection of Arf pathways by these inhibitors to best guide their use and development as therapeutic agents. Expand