Current Topics in Medicinal Chemistry - Volume 4, Issue 2, 2004

Transformation of a normal cell into a tumor cell results from six essential alterations in cell physiology. There is a complex relationship that exists between growth, differentiation, neoplastic transformation, and the expression of genes and tumor suppressor genes. The knowledge of these mechanisms demonstrates that it is possible to pharmacologically modulate the growth and differentiation of tumor cells. The differenti Read More

In the last two decades, paclitaxel (Taxol™, 1) has dominated the anticancer chemotherapy as one of the most important antimitotic agents. Despite its clinical success, it presents some limitations due to its low aqueous solubility or multidrug-resistance (MDR) susceptibility. Among new compounds sharing paclitaxel's mechanism of action, epothilones have emerged as very promising candidates and are currently under Read More

Aza-bioisosteres of anthracene-9,10-diones and of anthrapyrazoles comprise an innovative class of anticancer compounds. They are formally derived by introduction of one or more nitrogens into the carbocyclic ring system of the parent drugs. Bioisosteres exhibit extensive changes in the physico-chemical properties and in the interactions with the pharmacological targets, DNA and DNA-topoisomerase II, when compared t Read More

Analogues of naturally occurring antitumor agents, such as distamycin A, which bind in the minor groove of DNA, represent a new class of anticancer compounds currently under investigation. Distamycin A has driven researcher's attention not only for their biological activity, but also for its non intercalative binding to the minor groove of doublestranded B-DNA, where it forms strong reversible complex preferentially at th Read More

Cancer will be the major cause of death in the 21st century and natural products should provide novel and more effective anticancer agents. This review deals with new natural molecules liable to become anticancer drugs, as well as recent specific strategies for a selective treatment of cancer. The introduction presents the current state of the art on anticancer research. Beside, in the following subheadings we summarize our re Read More