Anticancer drug antitumor agent

Lipid dispersion formulations, such as oil in water emulsions and microemulsions, are attractive carriers for lipophilic and anticancer drugs. Antitumor agents show their therapeutic activities only in the restricted sites where intact agents reach after administration. In particular, several studies have reported the ability of emulsions to enhance the accumulation of anticancer agents into solid tumors compared to the free drug. Emulsions are considered superior due to their suitability for industrial scale production, stability on storage, biocompatibility, and the incorporation efficacy for lipophilic drugs. However, in practical terms, there... 

The renaissance of the Biginelli MCR can be attributed to the obtained pyrimidine derivatives, which show remarkable pharmacological activity. A broad range of effects, including antiviral, antitumor, antibacterial, anti-inflammatory as well as antihypertensive activities has been ascribed to these partly reduced pyrimidine derivatives [96], such as 9-117 and 9-118 (antihypertensive agents) [97] and 9-119 (ala-adrenoceptor-selective antagonist) [98] (Scheme 9.24). Recently, the scope of this pharmacophore has been further increased by the identification of the 4-(3-hydroxyphenyl)-pyrimidin-2-thione derivative 9-120 known as monastrol [98], a novel cell-permeable lead molecule for the development of new anticancer drugs. Monastrol appears specifically to affect cell division (mitosis) by a new mechanism,... 

Geiger T, Muller M, Dean NM, Fabbro D (1998) Antitumor activity of a PKC-alpha antisense oligonucleotide in combination with standard diemotherapeutic agents against various human tumors transplanted into nude mice. Anticancer Drug Des 13 35-45... 

The MTT assay was initially developed as a quantitative assay for cell survival and proliferation, not as an in vitro assay for chemosensitivity testing. Further study was required to ascertain if the method accurately predicted the in vivo antitumor activities of anticancer agents. Shimoyama et al. [189] studied the predictability of the MTT assay with respect to a clonogenic assay (Sect. 4.1.1.3.) and showed excellent reproducibility and a close correlation to the in vivo predictability rate of the clonogenic assay. Another study [190] also showed that the MTT assay closely approximated (90%) the clinical activity of anticancer agents. Many authors have since utilized the MTT assay to determine the efficacy of polymeric anticancer drug conjugates. 

Cultures consisting of cell suspensions may be used directly to determine the efficacy of macromolecular antitumor agents. For example, suspensions of L12 10 leukemia cells were used to show the activity of HPMA copolymer anticancer drug conjugates [39], The cells, while in exponential growth, were diluted in culture medium to produce a cell density of approximately... 

The book contains 22 chapters and is divided into six Parts. The first chapter is by Rosenberg who, in a very personal manner, describes the time from the discovery of cisplatin to its acceptance as an established anticancer drug in the late seventies. The chapter in Part 2, written by O Dwyer and colleagues, gives a topical account of the present clinical status of Pt antitumor agents. 

Hoes, H. P., Wagener, D.J., DE Valk-Bakker, V, VAN Rennes, H., de Vos, D., Doesburg, W.H., Ottenheijm, H.C., de Grip, W. J., Schedule-dependent enhancement of antitumor activity of ethyldeshy-droxy-sparsomycin in combination with dassical antineoplastic agents. Anticancer Drugs 1995, 6, 277-284. 

J. Reedijk and J. M. Teuben, Platmmn - Sulfur Interactions Involved in Antitumor Drugs, Rescue Agents, and Biomolecules, in 30 Years of Cisplatm, Chemistry and Biochemistry of a Leading Anticancer Drug , ed. B. Lippert, Wiley VCH, Weinheun, 1999, p. 339. 

Pt-BASED ANTITUMOR AGENTS See also Platinum-based Anticancer Drugs)... 

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