Evaluation of 2-(3-aminobenzamido)-2-deoxy-D-glucose as a radiosensitizer.

PURPOSE: 3-Aminobenzamide (3-AB), an inhibitor of poly(adenosine diphosphate [ADP]-ribose) synthetase, functions as a radiosensitizer in several human tumor cell lines. 2-(3-AB)-2-deoxy-D-glucose (3-AB-G) was designed to increase preferentially the intracellular concentration of the drug in tumor cells. Both the toxicity and effectiveness of 3-AB-G as a radiosensitizer were determined. MATERIALS AND METHODS: The toxicity of 3-AB-G was measured in HeLa and Chinese hamster ovary cells. The radiosensitizing effect of 3-AB-G was determined for both cell lines. RESULTS: 3-AB-G was not toxic to cells at concentrations of 10 mmol/L or less. 3-AB-G did not alter cell survival after irradiation. CONCLUSION: 3-AB-G was not an effective radiosensitizer for the cells tested. Coupling 2-deoxyglucose to 3-AB may block the uptake of the inhibitor into the cell by altering the ability of the receptor to recognize the molecule or may interfere with the specificity of the inhibitor for poly(ADP-ribose) synthetase.

Selenium heterocycles XXII: Synthesis and antibacterial antifungal activities of arylsulfonyl-1,2,3-selenadiazoles.

Series of 4-arylsulfonylmethyl-1,2,3-selenadiazoles, 4-(1-arylsulfonylethyl)-1,2,3-selenadiazoles, and 4-alkyl (or aryl)-5-arylsulfonyl-1,2,3-selenadiazoles were synthesized. 4-(3-Pyridyl)-5-phenylsulfonyl-1,2,3-selenadiazole exhibited the highest activity of growth inhibition against some bacteria and fungi.

Alkaloids of papaver genus IX. Alkaloids of Glaucium vitellinum Boiss and Buhse, population Seerjan and Glaucium pulchrum Stapf, population Elika.

Glaucium vitellinum Boiss and Buhse. population Seerjan was shown to contain three major alkaloids, isocorydine (0.44%), protopine (0.42%), dicentrine (0.24%), and four minor alkaloids, tetrahydropalmatine (0.13%), muramine (0.12%), bulbocapnine (0.06%) and glaucine (0.01%). Glaucium pulchrum Stapf popllation Elika was shown to contain two major alkaloids, corydine (0.3%) and bulbocapnine (0.18%) and three minor alkaloids N-methylindcarpine (0.1%), isocorydine (0.03%) and protopine (0.01%). N-methyllindcarpine was found for the first time in the Papaveraceae and tetrahydropalmatine was detected for the first time in Glaucium.

Alkaloids of Papaver orientale L.

According to the alkaloid profiles, five different chemotypes (A, B, C, D, and E) were classified in Papaver orientale L. with haploid chromosome number n = 14. Chemotype A had only oripavine; chemotype B contained oripavine and thebaine; chemotype C had isothebaine in addition to oripavine; chemotype D contained oripavine and alpinigenine; and chemotype E had oripavine, thebaine, and alpinigenine. In all chemotypes, oripavine was either the sole alkaloid or the single major alkaloid.

Major alkaloids of Glaucium flavum Grantz, population Ghom.

Glaucium flavum Grantz, population Ghom, contains 1.24% dicentrine, 0.89% bulbocapnine, and 0.05% salutaridine in dry aerial parts and root of the flowering plant. These alkaloids were detected for the first time in the Glaucium genus.

Selenium heterocycles XVIII: Synthesis and antibacterial activity of 4-substituted (1,2,3-selenadiazol-5-yl) carbamic acid esters and their sulfur analogs.

4-Substituted (1,2,3-selenadiazol-5-yl)carbamic acid esters and their sulfur analogs were prepared from the Curtius rearrangement of the corresponding carboxazides. None of the compounds showed significant antibacterial activity.

Alkaloids of Papaver orientale and papaver pseudo-orientale.

Dry latex of Paaver orientale was shown to contain 20% oripavine and 9% thebaine. Dry latex of Papaver pseudo-orientale contained two major alkaloids, isothebaine (11.7%) and orientalidine (0.5%), and the minor alkaloids bracteolin, salutaridine, Or1, Or2, PO-4, alborine (PO-5), and a novel alkaloid aryapavine.

Synthesis and evaluation of antitumor activity of 1-[N, N-bis(2-chloroethyl) sulfamoylphenyl]-3,3-dialkyltriazenes.

Twenty-two 1-p-sulfamoylphenyl-3,3-dialkyltriazenes, 1-p-dialkylsulfamoylphenyl-3,3-dialkyltriazenes, and 1-p-[N,N-bis(2-chloroethyl) sulfamoylphenyl] -3,3-dialkyltriazenes were synthesized from their corresponding amines. Six of the compounds tested were devoid of antitumor activity.