BACKGROUND C9, a newly in silico-designed inhibitor of microtubule dynamics induces G2/M arrest culminating in apoptosis. Dichloroacetate (DCA) inhibits pyruvate dehydrogenase kinase, an enzyme that promotes pyruvate entry into mitochondria. The use of antitumor drugs targeting different cancer features can be a more effective way to overcome drug resistance. METHODS The influence of C9 (130 ...

Previous studies of neural cell adhesion molecule (NCAM) cDNAs have revealed an alternatively spliced set of small exons (12A, 12B, 12C, and 12D) that encode a region in the extracellular portion of the molecule known as the muscle-specific domain (MSD). The entire MSD region can be expressed in skeletal muscle, heart, and skin; only exons 12A and 12D have been found in brain. These studies did...

A radiometric method for testing the susceptibility of Mycobacterium tuberculosis to pyrazinamide in egg-yolk-enriched 12A medium (pH 5.5) is described. We obtained 100% agreement between the 7H10 agar method with 25 microgram of pyrazinamide per ml and the modified radiometric method with a drug concentration of 50 microgram/ml in tests of 90 clinical isolates.

The dactylocycline antibiotics were found through circular dichroism measurements, NMR spectroscopy and chemical transformations to possess the usual tetracycline family absolute configuration at carbons 4, 4a, 5a and 12a. The absolute stereochemistry about the C-6 carbon, however, was the reverse of that found with previously investigated tetracyclines.

The straightforward synthesis of four gem-difluoromethylenated analogues 4-7 of boronolide is described. The key steps of the synthesis include the concise preparation of the key intermediates 12a-b through the indium-mediated gem-difluoropropargylation of aldehyde 9 with the fluorine-containing building block 11 and the efficient construction of alpha,beta-unsaturated-delta-lactones 15a-b via ...

Insects of the suborder Heteroptera are known for their odor, for being pests, or for being disease carriers. To gain better insight into the cytogenetic characteristics of heteropterans, 18 species of terrestrial Heteroptera belonging to eight families were studied. The presence of heteropycnotic corpuscles during prophase I, terminal or interstitial chiasmas, telomeric associations between ch...

The quaternary beta-carbolinium alkaloid nostocarboline from the cyanobacterium Nostoc 78-12A and 10 bis-cationic dimeric derivatives were evaluated against four protozoan parasites and low micromolar values against Trypanosoma brucei, submicromolar values against Leishmania donovani and low nanomolar values against Plasmodium falciparum K1 were determined. Selectivity against rat myoblasts (L6...

Background Severe liver damage like cirrhosis and hepatocellular carcinoma (HCC) can be caused by manifestation of the hepatitis C virus (HCV) infection. Constitutively activated c-Myc oncogene has been shown to contribute to the establishment of HCV-mediated HCC. Interestingly, only one of many isoforms of the tumor suppressor protein Bin1 (bridging integrator 1), Bin1+12A, contains an interna...