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Structure-based discovery of triphenylmethane derivatives as inhibitors of hepatitis C virus helicase.
TLDR
These inhibitors with structural novelty may serve as a useful scaffold for the discovery of new HCV NS3 helicase inhibitors and suppressed HCV replication in the HCV replicon cells.
Accelerated clearance of polyethylene glycol-modified proteins by anti-polyethylene glycol IgM.
TLDR
AGP3 clearance of betaG-sPEG before administration of BHAMG, a glucuronide prodrug of p-hydroxyaniline mustard, prevented toxicity associated with systemic activation of the prodrug based on mouse weight and blood cell numbers.
Investigation of anticancer mechanism of thiadiazole-based compound in human non-small cell lung cancer A549 cells.
TLDR
GO-13 is the most effective anticancer compound in the screening tests and showed equivalent anti-angiogenic activity in the nude mice angiogenesis model and is positively correlated with the increase in caspase-3 activity.
Efficient clearance of poly(ethylene glycol)-modified immunoenzyme with anti-PEG monoclonal antibody for prodrug cancer therapy.
TLDR
Treatment of nude mice bearing established human colon adenocarcinoma xenografts with B72.3-betaG-PEG followed 48 h later with AGP3 and a glucuronide prodrug of p-hydroxyaniline mustard significantly delayed tumor growth with minimal toxicity compared to therapy with a control conjugate or conventional chemotherapy.
Novel lead generation through hypothetical pharmacophore three-dimensional database searching: discovery of isoflavonoids as nonsteroidal inhibitors of rat 5 alpha-reductase.
TLDR
This investigation has demonstrated a practical approach toward the development of lead compounds through a hypothetic pharmacophore via three-dimensional database searching.
Bystander killing of tumour cells by antibody-targeted enzymatic activation of a glucuronide prodrug
TLDR
RHI-βG-PEG, formed by linking poly(ethylene glycol)-modified β-glucuronidase to Mab RH1, was employed to examine bystander killing of antigen-negative N1S1 rat hepatoma cells by activation of a glucuronide prodrug (BHAMG) at antigen-positive AS-30D rat hepatomas, showing that targeted activation of BHAMG kills bystander tumour cells in vivo.
NS5B RNA dependent RNA polymerase inhibitors: the promising approach to treat hepatitis C virus infections.
TLDR
This review summarizes the lead identification, structure activity relationship (SAR) studies leading to the most potent NS5B inhibitors with subgenomic replicon activity.
Expression of human malaria parasite purine nucleoside phosphorylase in host enzyme-deficient erythrocyte culture. Enzyme characterization and identification of novel inhibitors.
TLDR
Two novel potent inhibitors of both human erythrocyte and parasite purine nucleoside phosphorylase, 8-amino-5-deoxy-5'-chloroguanosine and 8-AMino-9-benzylguanine are identified and may have some antimalarial potential by limiting hypoxanthine production in the parasite-infected ery Throttle.
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential
TLDR
A series of 2-substituted methyl 2,3-dihydroimidazo[1, 2-c]quinazolin-5(6H)-ones, synthesized as compound 1conformational rigid congeners for pharmacological evaluation as potential alpha1-adrenoceptor antagonists, found that these compounds possessed weak to no activity against the 5-HT1A receptor.
Benzyl ether-linked glucuronide derivative of 10-hydroxycamptothecin designed for selective camptothecin-based anticancer therapy.
TLDR
A beta-glucuronidase-activated prodrug approach was applied to 10-hydroxycamptothecin, a Camptotheca alkaloid with promising antitumor activity but poor water solubility, and prodrug 7 was 10- to 15-fold less toxic than the parent drug to four human tumor cell lines.
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