Polymers Antineoplastic

Numerous antineoplastic polymers have been prepared with varying degrees of activity. For convenience, these polymers are divided here into (a) polyanions, (b) nucleic acid analogs, and... 

It is obvious that this approach using nucleic bases can lead to antineoplastic polymers since several such systems have shown this activity (34,45,46,48). This is not totally unexpected since the nucleic base derivatives 5-fluorouracll and 6-mercaptopurlne are antineoplastic agents. The polymers of this type made to date have been either the Insoluble type or the soluble type polymeric drug systems. This approach should be especially effective if some directing group is also put into these polymers to carry them selectively into tumorous tissue. Research along this line is in progress in our laboratories and some other places as well. 

Abstract Benzimidazoles, benzothiazoles and benzooxazoles are privileged structural units not only in the pharmaceutical industry but also in several other fields such as agricultural, electronic, and polymer chemistry. This ring system is present in numerous antioxidant, antiparasitic, antihelmintics, antiproliferative, anti-HIV, anticonvulsant, anti-inflammatory, antihypertensive, antineoplastic and antitrichinellosis activities. Owing to the immense importance of benzimidazoles, efforts have been made from time to time to generate various derivatives of these compounds. These methods have been well described in this Chapter. 

Use Medicine (antineoplastic), insect sterilant. Also used with tetrakis(hydroxymethyl)phosphonium chloride (THPC) to form a condensation polymer suitable for flame-proofing cotton. 

Gebelein and coworkers have prepared monomers and polymers based on the antineoplastic agents 5-fluorouracil and 6-mercapto-purine (26). These polymers would be potentially useful in treating various types of cancer or leukemia and some derivatives have shown biological activity. Previous work by this group has Included the synthesis of polyisoprene derivatives containing sulfa drug, carbamate, urea, oxazolldone and oxazole units (27.28). 

Many other polymers with antineoplastic properties have been prepared. For the most part, these polymers contain a known antineoplastic compound attached to the polymer chain as a pendant group. The earliest examples of this type seem to be the aziridine alkylating group containing polymers (XIX) (52), and (XX) (53), and (XXI) (54) which contains the cytostatic agent sarcolysin. 

The present, brief review clearly shows that several different types of polymers can exhibit antineoplastic activity. It is not possible, at the present time, to state with certainty which polymeric system(s) will eventually prove to be the most useful in cancer therapy, but a directed polymeric antineoplastic agent would probably be the most desirable, if such a system can actually be synthesized. Some of the areas highlighted in this review will be considered further In some of the subsequent chapters of this book. 

USE Insect chemosterilant in dyeing, creaseproofing and flameproofing textiles stabilizer for polymers in photographic emulsion hardening. therap cat Antineoplastic. 

This chapter explores the development of biodegradable polyanhydride polymers as a local chemotherapeutic delivery system in brain tumor patients. In so doing, the authors detail the unique pharmacokinetic considerations inherent in CNS drug delivery, and the resultant advantages of local administration. Subsequent sections chronicle the development of biocompatible technologies, preclinical and clinical experience with polymer-based tumor treatments, and potential future advancements in local antineoplastic drug delivery. 

Products of the reaction of K2PtCl4 with polymers are used similarly as the antineoplastic drug cw-dichlorodiamminoplatinum, for example for treatment of leukemia [80]. 

Malik, Duncan, Tomalia, and Esfand [29] reported the use of a variety of amine and acid-containing polymers that chelated platinum forming cisplatin derivatives. They also reported the synthesis of similar dendritic-antineoplastic drugs using vanadocene dichloride. The structure from the poly(propyleneimine) dendrimers contains units are shown in (5) and (6). 

Long chain polymer consisting of linear (1 ->4)-i>mannopyranosyl units, randomly acetylated (0.8 Ac per monomer) MW >10000 Dalton. Constit. of leaf juice of Aloe barbadensis and Aloe arborescens (Liliaceae). Biol, active component of carrisyn extract (73-90%). Potent inducer of Interleukin 1 and Prostaglandin E2 production by human peripheral blood adherent cells in vitro. Influences activity and production of T-lymphocytes, fibroblasts, B-lympho-cytes and endothelial cells. Adjuvant and immunoenhancer. Increases antibody production, stimulates phagocytosis. Shows specific antineoplastic activity against sarcoid tumours in horse. Used in the treatment of inflammatory bowel disease. Fluffy amorph. powder. 

Zamora and eo-workers employed the synthetic thio analog of the neutral purine hypoxanthine, 6-mercaptopurine (C5H4N4S, MP), to obtain a rich family of ID coordination polymers. 6-mercaptopurine (Fig. 21) has been studied for years because of its interesting applications as an antineoplastic (treatment of human leukemias), immunosuppressive and anti-inflammatory drug. This fact has motivated new research toward the synthesis and biological studies of metal coordination compounds based on MP. 

The soluble polymeric drugs differ from the insoluble type in that they are soluble in the body fluids. For this reason, these polymers could be administered orally or injected into the body and would not require surgery. These polymers could be homopolymers, such as poly(acrylic acid) or sodium poly(vinyl sulfonate) which show some antineoplastic activity, or they could be a copolymer which contains a drug unit and a second monomer whose primary function is to confer solubility on the copolymer system in the body fluids. These could be copolymers of a drug unit containing monomer with such comonomers as acrylic acid, N-vinylpyrrolidone, vinylamine oxides, vinyl sulfonate, vinyl imidazole or related monomers. Several examples of such systems have been prepared (5,6, 9-11). 

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