The pace of anticancer drug discovery and development has accelerated over recent years based upon a better understanding of tumour biology at the molecular level. Modern drug development has moved from empiricism to rational design and this was the theme of the inaugural meeting of the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics held in Washington DC, November 16 - 19.1999. This was an excellent meeting where state of the art research in the areas of drug discovery, development and clinical evaluation of new cancer therapeutics was presented. A few of the highlights of this meeting are presented in this article but further details can he found in a supplement to Clinical Cancer Research (1999) 5:3729-3897, where all abstracts accepted for the meeting are published. This meeting is set to become the premier meeting for scientists and clinicians involved in all aspects of anticancer drug development (i.e., from bench to the bedside) and the next meeting will take place in Amsterdam on November 7-10, 2000.