New small-molecule tubulin inhibitors*
G. Bacher, T. Beckers, P. Emig, T. Klenner, B. Kutscher, and B. Nickel
ASTA Medica AG, Research & Development Oncology,
Weismuellerstrasse 45, 60314 Frankfurt, Germany
Abstract: The variety of biological agents directed toward the
tubulin system exceeds those acting on DNA, making it an important target
for cancer chemotherapy. However, the complicated chemical structures
and restricted access to the natural resources, in combination with
the development of drug resistance, limit the first generation of natural
products. Considerable efforts in the search and synthesis of new synthetic
compounds, such as small molecular tubulin inhibitors, gave access to
novel potential/promising drugs. Among these substances, two series
of novel, easily accessible indole classes were identified as tubulin-destabilizing
agents. Owing to the synthetic nature, potent in vitro and in vivo antitumoral
activity, and efficacy against multidrug-resistant (MDR) tumors, D-24851
and D-64131 have significant potential in cancer treatment.
*Plenary lecture presented at the Hungarian-German-Italian-Polish
Joint Meeting on Medicinal Chemistry, Budapest, Hungary, 2 6 September
2001. Other presentations are published in this issue, pp.
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