Anita Tiwari

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Purpose: The purpose of this investigation was to compare the antitumor activities of a series of acyl derivatives of 4-demethylpenclomedine (DM-PEN), the major plasma metabolite of penclomedine (PEN) observed to be an active antitumor agent in vivo and non-neurotoxic in a rat model with that of DM-PEN. Methods: Acyl derivatives were prepared from DM-PEN(More)
S-adenosylmethionine decarboxylase (AdoMetDC) is a critical enzyme in the polyamine biosynthetic pathway and depends on a pyruvoyl group for the decarboxylation process. The crystal structures of the enzyme with various inhibitors at the active site have shown that the adenine base of the ligands adopts an unusual syn conformation when bound to the enzyme.(More)
Carbonic anhydrase (CA, EC: 4.2.1.1) activity in teak (Tectona grandis L.f.) was studied to determine its characteristics, kinetics and isozyme patterns. We also investigated effects of leaf age, plant age and genotype on CA activity and gas exchange parameters. Carbonic anhydrase extracted from leaves in 12 mM veronal buffer, pH 7.8, had a K(m) for CO(2)(More)
The main objective of this investigation was to identify the reactive pharmacophore in penclomedine (PEN, 3,5-dichloro-4,6-dimethoxy-2-(trichloromethyl) pyridine) for in vivo antitumor activity and also to discover related ring structures and sulfur analogues that might exhibit superior antitumor activity in vivo. Several new analogues of PEN and related(More)
Penclomedine [3,5-dichloro-4,6-dimethoxy-2-(trichloromethyl)pyridine], an antitumor agent, is currently in Phase I clinical trials and is believed to be a prodrug. In these studies, cerebellar effects have been dose limiting. Previous studies identified 4-demethylpenclomedine (4-DM-PEN) as the major plasma metabolite in rodents and humans. 4-DM-PEN was(More)
Analogues of penclomedine (PEN, 3,5-dichloro-4,6-dimethoxy-2-(trichloromethyl)pyridine) and its metabolites have been synthesized and evaluated as potential antitumor agents. PEN and 4-DMPEN (3,5-dichloro-4-hydroxy-6-methoxy2-(trichloromethyl)pyridine (3a)), the major plasma metabolite in patients, were modified at 4- and 6-positions with different alkyl,(More)
Seven new (2-chloroethyl)nitrosocarbamates have been synthesized as potential anticancer alkylating agents. These compounds were designed with carrier moieties that would either act as prodrugs or confer water solubility. All compounds were screened in an in vitro panel of five human tumor cell lines: CAKI-1 (renal), DLD-1 (colon), NCI-H23 (lung), SK-MEL-28(More)
Background: To determine if misoprostol use prior to intrauterine device (IUD) insertion decreases pain and eases insertion in nulliparous women. Study Design: Nulliparous women requesting IUDs for contraception were randomized to 400 micrograms of misoprostol or placebo prior to IUD insertion. The primary outcome was pain at the time of insertion using a(More)
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