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Relationships between hydrophobicity, reactivity, accumulation and peripheral nerve toxicity of a series of platinum drugs
TLDR
The hydrophobicity of platinum drugs correlates with platinum sequestration in the peripheral nervous system but not with neurotoxicity, and differences in the reactivity of platinum complexes accounts for some of the variation in their neurotoxicity. Expand
Gemcitabine sensitization by checkpoint kinase 1 inhibition correlates with inhibition of a Rad51 DNA damage response in pancreatic cancer cells
TLDR
The data suggest the inhibition of this Chk1-mediated Rad51 response to gem citabine-induced replication stress is an important factor in determining gemcitabine chemosensitization by Chk 1 inhibition in pancreatic cancer cells. Expand
Bioactivation of dinitrobenzamide mustards by an E. coli B nitroreductase.
TLDR
A series of compounds related to SN 23862 have been synthesized, and evaluated as potential prodrugs both by determination of kinetic parameters and by ratio of IC50 against UV4 cells when incubated in the presence of prodrug, with and without the E. coli nitroreductase. Expand
Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy.
TLDR
This study suggests that nitrogen mustard analogues derived from 5-(aziridin-1-yl)-2,4-dinitrobenzamide showed considerable improvements over 1, exhibiting greater potency, higher IC50 ratios, and lower TE50s, and are thus superior prodrugs to 1 for GDEPT. Expand
Effect of nitroreduction on the alkylating reactivity and cytotoxicity of the 2,4-dinitrobenzamide-5-aziridine CB 1954 and the corresponding nitrogen mustard SN 23862: distinct mechanisms of
TLDR
There was a highly significant linear relationship between cytotoxic potency and alkylating reactivity in both the aziridine and the mustard series, with the notable exception of 4, the 4-hydroxylamine of 1, which was 300-fold more toxic than predicted by this relationship. Expand
Thalidomide Pharmacokinetics and Metabolite Formation in Mice, Rabbits, and Multiple Myeloma Patients
TLDR
It is suggested that the interspecies differences in biological effects of thalidomide may be attributable, at least in part, to the differences in its metabolism and hence pharmacokinetics. Expand
Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug
TLDR
New heterocyclic analogues of the potent biphenyl class derived from antitubercular drug PA-824 were prepared, aiming to improve aqueous solubility but maintain high metabolic stability and efficacy, with examples from the latter classes displaying the better in vivo efficacies, high metabolic stabilities, and excellent pharmacokinetics. Expand
A revised biosynthetic pathway for the cofactor F420 in prokaryotes
TLDR
The structure of the guanylyltransferase FbiD is presented and it is shown that, along with its archaeal homolog CofC, it accepts phosphoenolpyruvate, rather than 2-phospho-l-lactate, as the substrate, leading to the formation of the previously uncharacterized intermediate dehydro-F420-0. Expand
Mechanisms and biomaterials in pH-responsive tumour targeted drug delivery: A review.
TLDR
P pH-responsive biomaterials bring forth conformational changes in these nanocarriers through various mechanisms such as protonation, charge reversal or cleavage of a chemical bond, facilitating tumour specific cell uptake or drug release, helping to design more efficient drug delivery systems. Expand
Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor
TLDR
A series of 6- and 7-acrylamide derivatives of the 4-(phenylamino)quinazoline and -pyridopyrimidine classes of epidermal growth factor receptor (EGFR) inhibitors showed significant tumor growth inhibition (stasis) over a dose range, and the poor aqueous solubility of the compounds was a drawback. Expand
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