Microtubule binders are cell cycle-specific agents with preferential cytotoxicity toward mitotic cells. We have characterized vincristine-selected human leukemia cells to establish whether development of vincristine resistance was accompanied by changes in cell cycle kinetics and distribution. Our results indicate that vincristine resistance is accompanied by delayed G2 transit and prolonged ea...

A new series of AT-specific minor groove DNA ligands (DB3P(n); n = 1,2,3,4) was synthesized and their spectral, biological virological properties were investigated. With a methylene spacers different lengths blocks three AT pairs located at distances from each other could be recognized. The compounds suppressed the activity HIV-1 integrase submicromolar concentrations (0.25–0.50 µМ). Also, DB3P...

As part of a series of studies to discover new topoisomerase II inhibitors, novel pyrimidoacridones, pyrimidophenoxadines, and pyrimidocarbazoles were synthesized, and in vitro and in vivo antitumor activities and DNA-protein and/or DNA-topoisomerase II cross-linking activity as an indicator of topoisomerase II-DNA cleavable complex formation were evaluated. The pyrimidocarbazoles possessed hig...