Anti-cancer therapeutics

Although the correlation between structural properties of aromatic hydrocarbons and their carcinogenic properties proved to be much more complicated than was hoped, this type of calculation opened the door to the application of quantum chemistry to biological systems. The calculations are applied not only to cancer-related problems, but also to the study of amino acids, peptides, nucleotides, and other than anti-cancer therapeutic agents. 

Board, R. and Jayson, G. 2005. Platelet-derived growth factor receptor (PDGFR) a target for anti cancer therapeutics. Drug Resistance Updates 8(1-2), 75-83. 

Borghouts, C Kunz, C., and Groner, B. (2005) Current strategies for the development of peptide-based anti-cancer therapeutics. J. Pept. Sci. 11,713-726. 

Baker, J.R., Jr. Quintana, A. Piehler, L. Banazak-Holl, M. Tomalia, D. Raczka, E. The synthesis and testing of anti-cancer therapeutic nanodevices. Biomed. Microdevices 2001, 3, 61-69. 

Kerbel, R. S. (1991) Inhibition of tumor angiogenesis as a strategy to circumvent acquired resistance to anti-cancer therapeutic agents, BioEssays 13, 31-36. 

Thus, one anti-cancer therapeutic strategy has been to use inhibitors of SKI. Preliminary studies in situ and in animal models indicate that SKI inhibitors prevent cancer cell proliferation and tumor growth (French et al.,... 

Fig. 16.4 Roles of ceramide and SIP in anti-cancer therapeutics. The cellular balance between ceramide in tumor samples and SIP is believed to determine the fate of cancer cells. Often, within a tumor, there are altered levels/accumulation of ceramide (such as low Cig-ceramide levels in HNSCC) and high SIP levels, which are often secreted into the serum at relatively high concentrations. This causes the metabolic balance to favor SIP resulting in a pro-survival outcome. However, new therapies are being explored to shift this balance in favor of ceramide. Ultimately, these new treatments are aimed at increasing ceramide levels while inhibiting SIP generation, secretion, or signaling through SlPRs...

Traditional approaches to discovering anti-cancer therapeutics relied on identifying agents that were anti-proliferative with little or no cytotoxicity to normal cells. This approach, while successful, has yielded mainly cytotoxic drugs. Plant-derived compounds such as paclitaxel (Taxol ) [3,4] and vinca alkaloids (vincristine) [5] are two examples (Figure 1) of commercially used drugs identified using this approach. Paclitaxel is a stabilizer of tubulin and is marketed as Taxol for the treatment of breast and other cancers [6]. 

Independently, Zhou and co-workers used the same approach in their synthesis of highly functionalized quinazolines as potential anti-cancer therapeutics. In one example, fusion of 2-amino-3,4,5-trimethoxybenzoic acid with formamide under thermal conditions gave the desired quinazolinone in 25% yield. A dibenzofliran quinazoline derivative produced using this process exhibited anti-proliferative properties against several tumor types, including Bcap-37, PC3, A431, and BGC823 cell lines. 

Benzimidazole derivatives as potential anticancer agents 13MRM399. Benzofuran-based estrogen receptor a modulators as anti-cancer therapeutics In sihco and experimental studies 13CMD2820. 

Multivalent glycidic constructs toward anti-cancer therapeutics... 

This review aims at giving a broad overview on the recent efforts in the design and synthesis of potentiai anti-cancer therapeutics based on muitivaient giycidic structures, covering iiterature up to 2013. 

Fischer PM, Lane DP. Inhibitors of cyclin-dependent kinases as anti-cancer therapeutics. Curr Med Chem 2000 7 1213-1245. 

Chk2 kinase, a tumor suppressor and key transducer of DNA damage checkpoints, plays a key role in blocking the cell cycle at various stages of mitosis, as well as inducing DNA repair and these molecules offer an attractive approach to the discovery of new targeted anti-cancer therapeutics. Select in vitro data will be presented to highlight the structure-activity relationships. 

Acknowledgement This work was supported by the National Research Foundation (NRF-2010-0000784), Ministry of Education, Science and Technology (MEST) in Korea. This work was also partially supported by the R D Program of MKE/KEIT (10035333, Development of anti-cancer therapeutic agent based on regulating cell cycle or cell death). 

Nitric Oxide Donors Are a New Class of Anti-cancer Therapeutics for the Reversal of Resistance and Inhibition of Metastasis... 

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