Anti-tumor compounds

Anti-tumor compound (205)-irinotecan (1) was prepared in 13 steps with an overall yield of 1.15 % for the longest linear synthesis. The short and selective preparation of aryl iodide 11 features two key steps - ortho metalation and Sharpless asymmetric dihydroxylation. In only one step 11 is transformed into the target molecule 1 by application of a radical domino annulation with isonitrile 15. This method gives access to the broad family of campthotecin derivatives because of the quite impressive generality of the substrates that can be employed. 

The development of tests that use cells cultured in vitro instead of animals could thus represent an important alternative in this area. Furthermore, the use of cell lines and primary tumor cells allows the evaluation of the potential of anti-tumor compounds with no need for inducing tumors in animals. The current protocols are well established for a variety of tumors, for instance in the National Cancer Institute of the USA. 

In searching for new structural variables for tin anti-tumor compounds, Gielen has proposed a number of perfluoroalkanecarboxylates, three of them being very active against seven tumor cell lines. His recent review on organotin compounds is an effort to systematize all kinetic and stereochemical evidence on most of their compounds with respect to results derived from cytotoxicity assays. ... 

ANTI TUMOR COMPOUNDS ISOLATED FROM HIGHER... 

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