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Your search keyword '"Mekapati, S. B."' showing total 3 results
Start Over Author "Mekapati, S. B." Journal bioorganic medicinal chemistry
3 results on '"Mekapati, S. B."'

1. QSAR of the inhibition of angiogenesis by TNP-470 and ovalicin analogues: another example of an allosteric interaction.

Author

Mekapati SB and Hansch C

Subjects
Aminopeptidases antagonists & inhibitors, Animals, Cattle, Cell Division drug effects, Cells, Cultured, Cyclohexanes, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Humans, Inhibitory Concentration 50, Lymphocytes drug effects, Metalloendopeptidases antagonists & inhibitors, Mice, O-(Chloroacetylcarbamoyl)fumagillol, Sesquiterpenes chemistry, Angiogenesis Inhibitors chemistry, Angiogenesis Inhibitors pharmacology, Quantitative Structure-Activity Relationship, Sesquiterpenes pharmacology
Abstract

QSAR have been formulated for variations of TNP-470 and Ovalicin on various cell lines. In the examples of mouse lymphocyte cells and bovine endothelial cells the results suggest an allosteric interaction. These results are compared with the binding of nitrobenzene to hemoglobin in rats in vivo. Such a reaction does not occur with methionine aminopeptidase.

Published
2001
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2. QSAR of anticancer compounds. Bis(11-oxo-11H-indeno[1,2-b]quinoline-6-carboxamides), bis(phenazine-1-carboxamides), and bis(naphthalimides).

Author

Mekapati SB, Denny WA, Kurup A, and Hansch C

Subjects
1-Naphthylamine analogs & derivatives, 1-Naphthylamine chemistry, Animals, Cell Division drug effects, Dimerization, Drug Screening Assays, Antitumor, Humans, Imides chemistry, Indenes chemistry, Inhibitory Concentration 50, Mice, Phenazines chemistry, Quinolines chemistry, Quinolones chemistry, Tumor Cells, Cultured drug effects, Antineoplastic Agents chemistry, Quantitative Structure-Activity Relationship
Abstract

QSAR have been developed for the anticancer activity (growth inhibition) of various tumor cells by bis(11-oxo-11H-indeno[1,2-b]quinoline-6-carboxamides), bis(phenazine-1-carboxamides), and bis(naphthalimides). Of the seven QSAR, positive hydrophobic interactions are found in only two examples: bis(naphthalimides) versus human colon cancer cells. This is consistent with other QSAR of anticancer compounds where hydrophobic interactions are found to be unimportant.

Published
2001
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3. Comparative QSAR studies on bibenzimidazoles and terbenzimidazoles inhibiting topoisomerase I.

Author

Mekapati SB and Hansch C

Subjects
Animals, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Cattle, DNA drug effects, DNA metabolism, Escherichia coli enzymology, Humans, Inhibitory Concentration 50, Tumor Cells, Cultured drug effects, Benzimidazoles chemistry, Benzimidazoles pharmacology, Quantitative Structure-Activity Relationship, Topoisomerase I Inhibitors
Abstract

Terbenzimidazoles that inhibit topoisomerase are of interest as anticancer drugs. We have reviewed the literature and have developed 13 quantitative structure-activity relationships (QSARs) on cleaving DNA or inhibiting the growth of tumor cell cultures. The results are correlated with octanol/water partition coefficients or molecular refractivity. Suggestions have been made for the development of improved derivatives.

Published
2001
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