As antitumor agents

Sucralfate [54182-58-0] an aluminum salt of sucrose octasulfate, is used as an antacid and antiulcer medication (59). Bis- and tris-platinum complexes of sucrose show promise as antitumor agents (60). Sucrose monoesters are used in some pharmaceutical preparations (21). A sucrose polyester is under evaluation as a contrast agent for magnetic resonance imaging (mri) (61). Oral adrninistration of this substance opacifies the gastrointestinal tract and eliminates the need for purging prior to mri. 

Bleomycin and cyclosporine are the two economically most important streptomycete peptide antibiotics used as antitumor agents and immunomodulators, although dactinomycin is important medically for several tumors (see Chemotherapeutics, anticancer Immunotherapeutic agents). 

Hansch and Verma contribute to the quantitative structure-activity relationship (QSAR) analysis of heterocyclic topoisomerase I and II inhibitors. These inhibitors, known to inhibit either enzyme, act as antitumor agents and are currently used in chemotherapy and in clinical trials. 

Petering DH, Antholine WE, Saryan LA (1984) In Ottenbrite RM, Butter GB (eds) Metal Complexes as Antitumor Agents in Anticancer and Interferron Agents, Marcel Dekker, NY, p 203... 

Presently there are two polyanionic polymers, MVE-2 and Carbetimer, that have undergone considerable clinical evaluation as antitumor agents. 

Nazarov, A. A. Dyson, P. J. Metal phosphorus complexes as antitumor agents. In Phosphorus Chemistry Catalysis and Material Science Applications, Vol. 37 (eds. Gonsalvi, L. Peruzzini, M.) 445-461 (Springer 2011). 

Jordan VC, Murphy CS (1990) Endocrine pharmacology of antiestrogens as antitumor agents. Endocr Rev 11 578... 

The dicytodendrins A-E (Fig. 9) are one of the most recent 3,4-diarylpyrrole natural products to be reported [64], Their isolation by Fusetani and coworkers from a Japanese marine sponge was reported in 2003. These substances (144-148) have been shown to inhibit telomerase at a concentration of 50 pg/mL thereby making such compounds potentially useful as antitumor agents given that telomerase activity is found in 90% of cancer cells but... 

Although a-carbolines (in particular, 2-amino-a-carboline) are perhaps better known as mutagens [89], some a-carbolines have been found to possess antitumor properties. For example, there has been much interest in the synthesis of natural products grossularine-1 133 and grossularine-2 134 (Fig. 38) since the report of their activity as antitumor agents at the 10 ng/mL level [90]. 

Synthetic a-carbolines have also attracted interest as antitumor agents. For example, Chen and coworkers [97] prepared a series of indolo[2,3-fr] quinoline derivatives, the most active of which was 154, which had a mean GI50 value against three cancer cell lines of 0.78 iM. This compound was prepared by methylation of 153 with dimethyl sulfate (Fig. 43), and was isolated in 12% yield, along with isomeric 155, which was isolated in 40% yield, but had significantly lower cytotoxicity. Precursor 153 itself was found to be inactive. 

Since natural product cryptolepine hydrochloride 173 (Fig. 48) has been found to be cytotoxic to B16 melanoma cells with an IC50 of 0.3 pg/mL (1.3 pM) [102], there has also been interest in cationic 5-carboline-based compounds as antitumor agents. For example, Wright and coworkers synthesized a series of these compounds and evaluated their activity against MAC 15 cells (murine adenocarcinomas of the colon) [103]. Of the compounds prepared, the most active was 179 which had an IC50 value of 1.03 pM. 

Inorganic or metal-containing medicinal compounds may contain either (a) chemical elements essential to life forms—iron salts used in the treatment of anemia—or (b) nonessential/toxic elements that carry out specific medicinal purposes—platinum-containing compounds as antitumor agents or technetium... 

Slichenmyer WJ, Rowinsky EK, Donehower RC, Kaufmann SH. The current status of camptothecin analogues as antitumor agents. J. Natl. Cancer Inst. 1993 Feb 17 85(4) 271-91. 

A and B, having detransformation activities as antitumor agents. Journal of Antibiotics (Tokyo), 43, 1524-1532. 

The disclosure of the HDLP crystal structure in 1999 provided a clear framework and starting point for medicinal chemists for the further development of HDAC inhibitors as antitumor agents. It confirmed the suggested general structural requirements of such inhibitors. These proposed requirements and the resemblance of the inhibitors to the acetylated e-amino groups of lysine residues are shown in Fig. 5. 

In Table 2 are shown the activities of (III), (IV) and (VI) under various conditions. The five other cyclophosphazenes, including the chlorine derivatives (I) and (II), were indeed found to be just at the limit of a significant activity (i.e., % ILS 25) within heavy Q4D (1, 5, 9, 13, 17) schedules. In other words, it is clear that the magic number assumption does not work as well as we could have expected however, NjPjQg and N P Clg must be considered as antitumor agents on P388, even if a repeated long polyinjection schedule is required to make their effectiveness conspicuous. 

Camptothecins as Antitumor Agents Clinical Pharmacology of the CPTs Interaction with Irradiation Topotecan Irinotecan... 

Susrni C, Buscail L. Rationale for the use of somatostatin analogs as antitumor agents. Aim Oncol 2006 17(12) 1733-42. 

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