An information-intensive approach to the molecular pharmacology of cancer

…, AP Monks, DA Scudiero, EA Sausville, DW Zaharevitz… - Science, 1997 - science.org
Since 1990, the National Cancer Institute (NCI) has screened more than 60,000 compounds
against a panel of 60 human cancer cell lines. The 50-percent growth-inhibitory …

Paullones are potent inhibitors of glycogen synthase kinase‐3β and cyclin‐dependent kinase 5/p25

…, P Greengard, DW Zaharevitz… - European journal of …, 2000 - Wiley Online Library
Paullones constitute a new family of benzazepinones with promising antitumoral properties.
They were recently described as potent, ATP‐competitive, inhibitors of the cell cycle …

Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity

C Schultz, A Link, M Leost, DW Zaharevitz… - Journal of medicinal …, 1999 - ACS Publications
… A presentation of the molecular modeling results and methods included in this paper is
accessible via the Internet from the following web site: Zaharevitz, DW; Gussio, R.; Leost, 2919 M.…

A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach

…, AR Hermone, JC Burnett, DW Zaharevitz… - Journal of medicinal …, 2005 - ACS Publications
Modulating the structure and function of tubulin and microtubules is an important route to
anticancer therapeutics, and therefore, small molecules that bind to tubulin and cause mitotic …

Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases

DW Zaharevitz, R Gussio, M Leost, AM Senderowicz… - Cancer research, 1999 - AACR
Abstract Analysis of the National Cancer Institute Human Tumor Cell Line Anti-Cancer Drug
Screen data using the COMPARE algorithm to detect similarities in the pattern of compound …

Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors.

…, DA Mitchell, W Furey, R Gussio, DW Zaharevitz… - Molecular …, 2002 - ASPET
Small molecules provide powerful tools to interrogate biological pathways but many
important pathway participants remain refractory to inhibitors. For example, Cdc25 dual-specificity …

COMPARE: a web accessible tool for investigating mechanisms of cell growth inhibition

DW Zaharevitz, SL Holbeck, C Bowerman… - Journal of Molecular …, 2002 - Elsevier
For more than 10 years the National Cancer Institute (NCI) has tested compounds for their
ability to inhibit the growth of human tumor cell lines in culture (NCI screen). Work of Ken Paull …

Identification of small molecule inhibitors of anthrax lethal factor

…, S Little, EA Sausville, DW Zaharevitz… - Nature structural & …, 2004 - nature.com
The virulent spore-forming bacterium Bacillus anthracis secretes anthrax toxin composed of
protective antigen (PA), lethal factor (LF) and edema factor (EF). LF is a Zn-dependent …

Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity

…, DJ Lane, EA Sausville, DW Zaharevitz… - Biochemical and …, 2003 - Elsevier
Botulinum neurotoxins (BoNTs) are among the most lethal biological substances to have
been weaponized and are listed as biodefense category A agents. Currently, no small …

Enhancement of the biological activity of adenosine analogs by the adenosine deaminase inhibitor 2'-deoxycoformycin

RH Adamson, DW Zaharevitz, DG Johns - Pharmacology, 1977 - karger.com
The potent adenosine deaminase inhibitor 2’-deoxycoformycin ((R)-3-(2-deoxy-β-i3-erthyropentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol)
inhibits the enzymic …