Electronic Resource
1 Topics in Medicinal Chemistry : Cancer
After over half a century of chemotherapy research, cancer remains one of the most difficult life-threatening diseases to treat, a consequence of factors which include limitations of animal models, tumour diversity, drug resistance and side effects of therapy. This introductory overview gives a brief perspective on the discovery of historical cytotoxic and anti-hormonal drugs, and then highlights the shift in research emphasis over the last 15 years towards agents that aim to selectively target regulatory and signalling processes known to drive tumourigenesis. Experience with newer drugs like imatinib (GLEEVEC™) is providing growing insight into the role of patient selection, design of clinical trials and mechanisms of drug resistance, and is also beginning to fulfil the anticipation that such agents could offer a more manageable side-effect profile than cytotoxic therapy. For medicinal chemists, the aims of anti-cancer drug discovery programmes have come more into line with other areas of drug therapy, with emphasis moving more towards orally bioavailable drugs with pharmacokinetics suitable for dosing once or twice a day, and with a property profile that not only limits toxic effects on proliferating tissue such as bone marrow but also minimises risks due to effects such as cardiac arrhythmia potential, cytochrome P450 liability and variable absorption. This volume reviews medicinal chemistry approaches to small molecule inhibitors of some key cellular regulatory and signalling networks, which have the potential to follow drugs like imatinib into clinical practice.
EBK-00233 | 615.1/Bra-t | Perpus Pusat | Tersedia |
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