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Investigation of anti-leukemia molecular mechanism of ITR-284, a carboxamide analog, in leukemia cells and its effects in WEHI-3 leukemia mice.
TLDR
Investigation of the underlying molecular mechanisms in vitro and in vivo of ITR-284 revealed that it acted against both HL-60 and WEHI-3 in vitrovia both intrinsic and extrinsic apoptotic signaling pathways, and exhibited an anti-leukemic effect in a THE AUTHORS HI-3 orthotopic mice model of leukemia. Expand
A Highly diastereoselective synthesis of (1R)-(+)-camphor-based chiral allenes and their asymmetric hydroboration-oxidation reactions.
TLDR
Reaction of (1R)-(+)-camphor with alkynyllithium followed by the reduction of the resulted propargyl alcohol derivatives using AlH3 furnished chiral allenes 2a-g in excellent yields with high diastereoselectivity are described. Expand
Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.
TLDR
Analogue 22 was identified from this series of azulene-based derivatives and found to be one of the most potent FLT-3 inhibitors, with good pharmaceutical properties, superior efficacy, and tolerability in a tumor xenograft model. Expand
Cell differentiation enhancement by hydrophilic derivatives of 4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-diones in HL-60 leukemia cells.
TLDR
Two ester-type hydrophilic prodrugs are identified in this paper as new anti-leukemic drug candidates and exhibited excellent and equally potent differentiation effects on HL-60 cells. Expand
Arsenic trioxide (As2O3) inhibits murine WEHI‐3 leukemia in BALB/c mice in vivo
TLDR
As 2O3 alone or As2O3 combined with ATRA have efficacious antileukemia activity in WEHI‐3 cells leukemia in vivo, indicating that the differentiation of T and B cells were promoted. Expand
2-(1-Hydroxethyl)-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione (BTP-11) enhances the ATRA-induced differentiation in human leukemia HL-60 cells.
TLDR
Western blot analysis revealed that combination of BTP-11 and ATRA decreased cyclin D/CDK4 and increased C/EBPvarepsilon protein expression to arrest the cells into G0/G1 phase leading to granulocytic maturation, and confirmed that B TP-11 is a potent enhancer for ATRA-induced differentiation of HL-60 cells. Expand
Carboxamide analog ITR-284 evokes apoptosis and inhibits migration ability in human lung adenocarcinoma A549 cells.
TLDR
The data suggest that ITR-284 may be an effective anticancer agent for treating lung adenocarcinoma. Expand
The novel carboxamide analog ITR-284 induces caspase-dependent apoptotic cell death in human hepatocellular and colorectal cancer cells.
TLDR
Investigation of the antiproliferative effects and apoptotic induction of ITR-284 on various types of human hepatocellular and colorectal cancer cells in vitro found that it induced apoptosis in Hep 3B and COLO 205 cells through the caspase cascade-dependent signaling pathway. Expand
Design and synthesis of new 2-arylnaphthyridin-4-ones as potent antitumor agents targeting tumorigenic cell lines.
TLDR
Among the above-mentioned target compounds, 2-(3-hydroxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (7a) demonstrated the greatest potency and the best selectivity toward tumorigenic cancer cell lines. Expand
ITR‑284 modulates cell differentiation in human chronic myelogenous leukemia K562 cells.
TLDR
The data show that I TR‑284 induced K562 cell differentiation, which led to decreased tumorigenesis, and suggest that ITR‑284 could be a potential candidate for treating chronic myelogenous leukemia. Expand