Thiosemicarbazones anticancer activity

Patole, J. Padhye, S. Padhye, S. Newton, C. J. Anson, C. Powell, A. K. Synthesis, characterization and in vitro anticancer activities of semicarbazone and thiosemicarbazone derivatives of salicylaldehyde and their copper complexes against human breast cancer cell line MCF-7. Indian J. Chem., Sect. A 2004, 43A, 1654-1658. 

French and Blanz [9-13] extended these observations by testing a series of formyl heteroaromatic thiosemicarbazones for anticancer activity several of these derivatives, especially 1-formylisoquinoline thiosemicarbazone [10], 2-formyl-3-hydroxypyridine thiosemicarbazone [11] and 2-formyl-5-hydroxy-pyridine thiosemicarbazone [13] showed significant tumour-inhibitory activity when tested against a spectrum of transplanted murine neoplasms. 

Anticancer examples, Thiosemicarbazones have been mentioned above in connexion with their antiviral and antitubercular properties. They also have anticancer activity, as already mentioned for 5-hydroxypicolinic aldehyde thiosemicarbazone (4.18) in Section 4.0. Such substances powerfully inhibit ribonucleoside diphosphate reductase, the enzyme which converts ribo- to deoxyribo- nucleotides, leading to inhibition of DNA synthesis. Interaction with the enzymatically-required iron by these drugs in thought to lie at the root of their action (Agrawal, et al,y 1972). 

Bis(thiosemicarbazones) [89-97] and AT-heterocyclic thiosemicarbazones comprise two interesting series of experimental chemotherapeutic agents. 2-formylpyridine thiosemicarbazone, the first of the latter series to be examined for biological activity, showed mild antileukemic activity against 1-1210 tumor in mice [98]. However, it was found to be toxic at the therapeutic dose levels which led to synthesis of other aromatic and heterocyclic thiosemicarbazones as potential agents [80, 99, 100]. However, the only active anticancer compounds besides glyoxal bis(thiosemicarbazones) were the iV-heterocyclic thiosemicarbazones [101], 2 formyl-3-hydroxypyridine thiosemicarbazone [102] and... 

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