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Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy.
TLDR
A small-molecule Bcl2-BH4 domain antagonist, BDA-366, that binds BH4 with high affinity and selectivity is identified that exhibits strong synergy against lung cancer in vivo. Expand
Fragment-based drug design and identification of HJC0123, a novel orally bioavailable STAT3 inhibitor for cancer therapy.
TLDR
The fragment-based drug design, systematic chemical synthesis and pharmacological evaluation of novel scaffolds as potent anticancer agents by utilizing six privileged fragments from known STAT3 inhibitors are reported, indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy. Expand
Small Molecule Bax Agonists for Cancer Therapy
TLDR
The structural pocket around S184 is employed as a docking site to screen the NCI library of small molecules using the UCSF-DOCK program suite and offers a strategy for the treatment of lung cancer and other Bax-expressing malignancies. Expand
Novel nitrogen-enriched oridonin analogues with thiazole-fused A-ring: protecting group-free synthesis, enhanced anticancer profile, and improved aqueous solubility.
TLDR
These new analogues obtained by rationally modifying the natural product have been demonstrated not only to significantly induce the apoptosis and suppress growth of triple-negative MDA-MB-231 breast cancer both in vitro and in vivo but also effective against drug-resistant ER-positive MCF-7 clones. Expand
Oridonin ring A-based diverse constructions of enone functionality: identification of novel dienone analogues effective for highly aggressive breast cancer by inducing apoptosis.
TLDR
These new analogues have been demonstrated to significantly induce apoptosis and inhibit colony formation with superior antitumor effects against aggressive and drug-resistant breast cancer cells in vitro and in vivo while also exhibiting comparable or lower toxicity to normal human mammary epithelial cells in comparison with 1. Expand
ent-Kaurane-based regio- and stereoselective inverse electron demand hetero-Diels-Alder reactions: synthesis of dihydropyran-fused diterpenoids.
TLDR
Efficient cross-HDA cycloadditions of this enone with various vinyl ethers or vinyl sulfides were achieved in a regio- and stereoselective manner, thus providing access to novel dihydropyran-fused diterpenoids as potential anticancer agents to overcome chemoresistance. Expand
Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist.
TLDR
A concise and efficient synthetic approach to producing a novel non-cyclic nucleotide EPAC antagonist ESI-09 and its new analogs is reported, requiring inexpensive starting materials and only three linear steps for the completion in a total yield of 53%. Expand
Enhanced effects of novel oridonin analog CYD0682 for hepatic fibrosis.
TLDR
In comparison with oridonin, its novel derivative CYD0682 may act as a more potent antihepatic fibrosis agent. Expand
Enhanced anti-fibrogenic effects of novel oridonin derivative CYD0692 in hepatic stellate cells
TLDR
The results indicated that pretreatment with CYD0692 blocked TGFβ1-induced FN expression, thereby decreasing the downstream factors of TGF β1 signaling, such as Phospho-Smad2/3 and phospho-ERK. Expand
Modulation of Bax and mTOR for Cancer Therapeutics.
TLDR
The refinement of the Bax agonist SMBA1 to generate CYD-2-11, which has characteristics of a suitable clinical lead compound and provides preclinical evidence for a pharmacologic combination of Bax activation and mTOR inhibition as a rational strategy to improve lung cancer treatment. Expand
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