Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines

Jennifer Dourlat; Wang-Qing Liu; Nohad Gresh; Christiane Garbay

doi:10.1016/j.bmcl.2007.02.016

Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines

Bioorg Med Chem Lett. 2007 May 1;17(9):2527-30. doi: 10.1016/j.bmcl.2007.02.016. Epub 2007 Feb 9.

Authors

Jennifer Dourlat¹, Wang-Qing Liu, Nohad Gresh, Christiane Garbay

Affiliation

¹ Université Paris Descartes, UFR Biomédicale, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, Paris F-75006, France.

PMID: 17317183
DOI: 10.1016/j.bmcl.2007.02.016

Abstract

Novel 1,4-benzodiazepine compounds were synthesized and evaluated for their ability to inhibit the proliferation of tumor cells. Some compounds revealed activities in the micromolar range and were more efficient than reference compound Ro 5-4864. Preliminary SAR helped to identify critical motifs for antiproliferative activity and led to the discovery of a compound selective for a melanoma cell line, known for its resistance to chemotherapy.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Benzodiazepines / chemical synthesis*
Benzodiazepines / pharmacology
Benzodiazepinones / pharmacology
Cell Line, Tumor
Cell Proliferation / drug effects*
Chemistry, Pharmaceutical / methods
Drug Design
Drug Resistance, Neoplasm*
Drug Screening Assays, Antitumor
Humans
Inhibitory Concentration 50
Melanoma / drug therapy
Models, Chemical
Molecular Conformation

Substances

Antineoplastic Agents
Benzodiazepinones
Benzodiazepines
4'-chlorodiazepam
Bz-423