Cancerostatic activity

So far, not much literature on the biological activity of iminophosphor-anes has appeared. Compounds possessing triorganylphosphoranylidenea-mino structural elements such as mitomycin (41) have proved to be interesting anti-tumor reagents the cancerostatic activity seems to be localized in the aziridine units of 40 (Scheme 19) [87PS(30)845]. 

Regarding the position of the central metal atoms in the Periodic Table, a diagonal relation Ti - Nb and V - Mo is obvious of those metals which display as central atoms in metallocene dichlorides marked cancerostatic activity ( ). This corresponds to... 

A racemic derivative (331) of crotepoxide, a naturally occurring branched-chain dianhydroinositol exhibiting cancerostatic activity, has been synthesized from 2-hydroxymethyl-l,4-benzoquinone by the route outlined in Scheme 118. ... 

After intravenous or oral administration of the drug, it undergoes several biotransformations that activate its toxicity (tumor cells as well as nephro- and neurotoxicity). A number of speciation studies that focused on characterization and quantification of parent drug and its possible metabohtes in vitro and in vivo have been reported. Element-specific ICP-MS detection has been applied after LC separation of platinum compounds. In Figure 6, the LC-ICP-MS chromatogram is presented, and this was obtained for the mixture of cancerostatic platinum compounds. ... 

A very intense search for antiviral and cancerostatic agents has led to the synthesis of countless nucleoside analogues. Virtually all possible chemical modifications (on the bases, sugars, and even the phosphate) have been made and tested in vitro and in vivo. Two of the most intensively studied antimetabolites are arabinosyl cytosine (araCyd) and formycin A (see Fig. 3-1). The former is used in the clinical treatment of oncogenic viruses and leukemia. After transformation to the triphosphate it is incorporated into DNA, where it may be a chain terminator. Formycin A and B (A is the Ado analogue, B the Ino analogue) are both in the syn conformation and have strong antiviral activity. 

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