Systemic cytotoxic (anti-proliferative) anticancer drugs rely primarily for their therapeutic
effect on cytokinetic differences between cancer and normal cells. One approach aimed at …

Acridine derivatives are one of the oldest classes of bioactives, widely used as antibacterial
and antiprotozoal agents. Some work in these areas continues, but recent research has …

This review provides an update on the mutagenicity of intercalating chemicals, as carried out
over the last 17 years. The most extensively studied DNA intercalating agents are acridine …

A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate
the epidermal growth factor receptor tyrosine kinase through specific, covalent modification …

Identifying new targeted therapies that kill tumor cells while sparing normal tissue is a major
challenge of cancer research. Using a high-throughput chemical synthetic lethal screen, we …

A series of substituted 2-phenylbenzimidazole-4-carboxamides has been synthesized and
evaluated for in vitro and in vivo antitumor activity. These compounds represent the logical …

4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (32, PD 153035) is a very potent inhibitor (IC
50 0.025 nM) of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR), …

4-Anilinoquinazoline- and 4-anilinopyrido[3,2-d]pyrimidine-6-acrylamides substituted with
solubilizing 7-alkylamine or 7-alkoxyamine side chains were prepared by reaction of the …

Squirrel monkeys have high circulating cortisol to compensate for expression of low-affinity
glucocorticoid receptors (GRs). We have demonstrated that the FK506-binding immunophilin …

A series of 4-substituted quinazolines and related compounds have been prepared and
evaluated for their ability to inhibit the tyrosine kinase activity of the epidermal growth factor …