Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 9, Issue 3, 2009

In the present review, the discovery and development of quinazoline as tyrosine kinase inhibitors has been described. The synthesis of most potent quinazoline inhibitors of EGFR, VEGFR and PDGRF has been discussed. Structure activity relationship for quinazoline as tyrosine kinase inhibitors has been established. It was found that C-4, C-6 and C-7 positions in quinazoline are appropriate sites for designing new tyrosine kinase inhib Read More

Available chemotherapeutics take advantage of the fast proliferation of cancer cells. Consequently slow growth makes androgen refractory prostate cancer resistant towards available drugs. No treatment is available at the present, when the cancer has developed metastases outside the prostate (T4 stage). Cytotoxins killing cells irrespective of the phase of the cell cycle will be able to kill slowly proliferating prostate cance Read More

Quantum dots (QDs) are fluorescent inorganic nanocrystals with advantageous optical properties, which have been applied for biomedical purposes including imaging, diagnostic, drug delivery or therapy. Potential toxicity of QDs remains the major barrier to clinical translation, and as such the precise analysis of in vivo QDs distribution and pharmacokinetics is of major importance. Biodistribution studies in animal models are, ho Read More

In recent years, a series of new and highly cytotoxic analogues of CC-1065 and the duocarmycins have been developed that can be transformed into much less toxic prodrugs for the use in antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT) and prodrug monotherapy (PMT) of cancer. In all these approaches, a relatively non-toxic prodrug is applied and subsequently converte Read More

Bone metastases are common in the event of malignancy and are inevitably associated with serious complications that may deteriorate the quality of life (QOL) of patients and threaten life. Both radiotherapy (RT) and bisphosphonates (BPs) have an established role in the management of metastatic bone disease. Many clinical trials have demonstrated their effectiveness when used as sole treatment modalities, but only a f Read More

The development of chalcones as antimitotic agents has led to the design of other analogues able to interact with tubulin and inhibit its assembly into microtubules. This activity has also been associated with their anti-vascular activity. This review focuses on the development of chalcones and related analogues as antimitotic agents.

Amplification of the HER2/neu gene occurs in approximately 20-25% of invasive breast cancers and is associated with poor patient outcome. The development of trastuzumab, a humanized monoclonal antibody that binds to the extracellular domain of HER2, has led to a significant improvement in outcomes of patients with HER2-positive breast cancer. However, many patients with HER2- positive metastatic breast c Read More

Research has proven that the most effective and widely used metal-containing chemotherapy anticancer drugs are cisplatin ([cis-PtCl2(NH3)2]) and many platinum complexes, however, these compounds have significant disadvantages including poor water solubility and serious side effects. Thus researches in order to overcome these shortcomings have never interrupted. Many non-platinum complexes have been synthesized and Read More