Silicon ‐containing analogs of camptothecin as anticancer agents

Abstract The plant pentacyclic alkaloid camptothecin and its structural analogs were extensively studied. These compounds are interesting due to the antitumor activity associated with their ability to inhibit topoisomerase I in tumor cells. During the last decades of the 20th century, a large number of the silicon‐containing camptothecins (silatecans) were synthesized. 7‐tert‐Butyldimethylsilyl‐10‐hydroxy‐camptothecin (DB‐67 or AR‐67) has enhanced lipophilicity and demonstrates a antitumor activity superior to its carbon analog. To date, certain silatecans are under clinical trials and their ultimate role in cancer therapy appears promising. In this review, we present chemical methodologies for the synthesis of silicon‐containing camptothecins, their chemical properties, biological activity, and results of clinical trials. During the last decades of the 20th century, many silicon‐containing camptothecins (silatecans) were synthesized. To date, certain silatecans are investigated in clinical trials and their role in cancer therapy appears promising. In this review, chemical methodologies for the synthesis of silicon‐containing camptothecins, their chemical properties, biological activities, and results of clinical trials are presented.
Source: Archiv der Pharmazie - Category: Drugs & Pharmacology Authors: Tags: REVIEW ARTICLE Source Type: research