Alkylating agents platinum complexes

The growth of a single cancer cell into a fully-developed tumour can be disrupted by cytostatics at a number of development stages. Important intervention points, each targeted by one or several classes of cytostatics, are the replication of DNA (alkylating agents, platinum complexes), cell division (antitubulin... 

The use of this phosphine facilitates assignment of configuration as virtual coupling is observed when the phosphines are trans (section 2.9.5).) Syntheses follow established routes using methyllithium as an alkylating agent the platinum(iV) complexes can be made by direct alkylation of platinum(IV) compounds or by oxidative addition to platinum(II) species. 

Alkylating agents Nitrogen mustards (cyclophosphamide) Busulphan Platinum coordination complexes (cisplatin) Nitrosoureas Crosshnks DNA strands... 

Heavy metal compounds used to treat cancer include cisplatin, carboplatin, and oxaliplatin (see Table 36-6). These drugs, which contain platinum, are also known as platinum coordination complexes.10,27 Heavy metal drugs act like the alkylating agents that is, they form strong cross-links between and within DNA strands,... 

Alkylating agents and related compounds act by forming covalent bonds with DNA. thus impeding DNA replication. They can be divided into five subgroups (i) nitrogen mustards (e.g. chlorambucil, cyclophosphamide, melphalan and mustine (ii) platinum drugs (coordination complexes of platinum) (e.g. cisplatin and carboplatin) ... 

Table 3. The effect of different classes of anti-tumour agent on some transplanted tumours. The TLX5 (R) is a line with acquired resistance to a triazene and is cross resistant to BCNU. Triazenes and BCNU are active against tumours which do not respond to anti-metabolites and others that are insensitive to alkylating agents. The platinum complex was cis dichloro-bis(cyclopentylamine)platinum(II) and the triazene 5-(3,3-dimethyl-l-triazeno)-4-carbethoxy-2-me thy limidazole...

Increased activity of DNA repair pathways, which may differ for the various alkylating agents. Thus, increased activity of the complex nucleotide excision repair (NER) pathway seems to correlate with resistance to most chloroethyl and platinum adducts. Alkyl guanine transferase (AGT) activity determines response to BCNU and to methylating drugs such as the triazenes, procarbazine, and busulfan ... 

The drug essentially cross-links DNA and, therefore, behaves like alkylating antineoplastic agents. In general, the platinum complex acts as apotent inhibitor of DNA polymerase. Based on adequate... 

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