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Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.
TLDR
Compound 4 was rapidly converted into 1 following iv and po administration and also possessed excellent antitumor activity in a SKOV-3 xenograft nude mice model and is highly promising for development as an anticancer clinical trials candidate. Expand
Specific microtubule-depolymerizing agents augment efficacy of dendritic cell-based cancer vaccines
TLDR
Specific MDAs including the clinical drug, colchicine, can induce immunogenic cell death in tumor cells, and DCs pulsed with MDA-treated tumor cell lysates (TCLs) can generate potent anti-tumor immunity in mice. Expand
Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agents.
TLDR
Sodium 2-(3-fluorophenyl)-5-hydroxy-6-methoxy-4-oxo-1,4-dihydroquinolin-5-yl phosphate (15), the monophosphate of 3b, exceeded the activity of doxorubicin and was comparable to CHM-1-P-Na in a Hep3B xenograft nude mice model. Expand
Synthesis of furopyrazole analogs of 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole (YC-1) as novel anti-leukemia agents.
TLDR
Through investigation of action mechanism, 1-benzyl-3-(substituted aryl)-5-methylfuro[3,2-c]pyrazole is identified here as a new lead compound of cell differentiating agent and apoptosis inducer for further development of new anti-leukemia agents. Expand
The synthesized 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one (CHM-1) promoted G2/M arrest through inhibition of CDK1 and induced apoptosis through the mitochondrial-dependent pathway in CT-26
TLDR
Taken together, CHM-1 acted against colorectal adenocarcinoma cells in vitro via G2/M arrest and apoptosis, and CHm-1-P inhibited tumor growth in vivo. Expand
Synthesis of 1-benzyl-3-(5-hydroxymethyl-2-furyl)selenolo[3,2-c]pyrazole derivatives as new anticancer agents.
TLDR
It is recommended that compound 2 should be developed further as new drug candidate for treatment of non-small cell lung cancer and renal cancer, and seems to differ from those of the 175 anticancer agents listed in NCI's standard database. Expand
CHM-1 induces apoptosis via p38-mediated upregulation of DR5 expression in human ovarian cancer SKOV3 cells.
TLDR
MTT assay was used to evaluate the antiproliferative effect of the 2-(substituted phenyl)-6,7-methylenedioxyquinolin-4-one derivatives for developing new anti-ovarian cancer drugs, and CHM-1 was the most active compound, and it exhibited potent antiprolifierative activity against human ovarian cancer cells. Expand
Synthesis and in vitro anticancer activity of 6,7-methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-one analogs.
TLDR
6,7-Methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-ones and their isosteric compounds were synthesized and evaluated for anticancer activity, finding 4d to be the most promising anticancer agent. Expand
Synthesis and SAR studies of novel 6,7,8‐substituted 4‐substituted benzyloxyquinolin‐2(1H)‐one derivatives for anticancer activity
TLDR
Four new 4‐Phenylquinolin‐2(1H)‐one derivatives can induce cancer cell apoptosis and were investigated as more effective, less toxic antitumour agents. Expand
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