Drugs antitumoral

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... 

Antineoplastic Drugs. Cyclophosphamide (193) produces antineoplastic effects (see Chemotherapeutics, anticancer) via biochemical conversion to a highly reactive phosphoramide mustard (194) it is chiral owing to the tetrahedral phosphoms atom. The therapeutic index of the (3)-(-)-cyclophosphamide [50-18-0] (193) is twice that of the (+)-enantiomer due to increased antitumor activity the enantiomers are equally toxic (139). The effectiveness of the DNA intercalator dmgs adriamycin [57-22-7] (195) and daunomycin [20830-81-3] (196) is affected by changes in stereochemistry within the aglycon portions of these compounds. Inversion of the carbohydrate C-1 stereocenter provides compounds without activity. The carbohydrate C-4 epimer of adriamycin, epimbicin [56420-45-2] is as potent as its parent molecule, but is significandy less toxic (139). 

Mitochondrial monoamine oxidase, 1, 253 Mitomycin synthesis, 7, 658, 659 Mitomycin-A, 7, 93 Mitomycin-B, 7, 93 Mitomycin-C, 7, 93 as antitumor drug, 4, 374 Mixed function oxidases, 1, 224 Mobam... 

A new antitumor drug, taxol, has been isolated from the bark of Taxus brevifolia, the Pacific yew tree. Like vinblastine and colchicine, taxol inhibits cell replication by acting on microtubules. Unlike these other antimitotic drugs, however, taxol stimulates microtubule polymerization and stabilizes microtubules. 

DNA cross-linking agents (mainly heterocycles) as antitumor drugs 98CRV2723. 

Natural and synthetic heterocycles as DNA cross-linking agents and antitumor drugs 98CRV2723. 

Pt-complexes with heterocyclic ligands and Pt-chelates as antitumor drugs 99CRV2451. 

As noted above, the steroid nucleus has been a favorite for the design for site directed alkylating antitumor drugs. Thus reaction of prednisolone (62) with anhydride 63 affords the 21 acylated derivative, prednimustine (64). ... 

German investigators (Brock et al) worked on the creation of alkylating pro-drugs that have cytostatic activity after specific biotransformation in the tumor tissue. Cyclophosphamide (CTX) has well pronounced antitumor activity with the broadest spectrum. It is metabolized to the cytotoxic phosphoamide mustard. In normal tissues with high enzyme level cyclophosphamide is converted to its inactive metabolites (Fig. 2). These differences in biotransformation can explain the relative selectivity of cyclophosphamide towards... 

Anticancer diugs Cytostatic drugs Cytotoxic drags Antitumor drags... 

Drugs (e.g., polynucleotides [e.g., polyriboinosinic polyribocytidylic acid], antitumor agents [e.g., bleomycin], plant alkaloids [e.g., colchicine], synthetic immunoadjuvants [e.g., muramyl peptides]... 

Bryostatins are another class of compounds that bind to the Cl domain and result in acute activation of PKC. However, unlike phorbol esters, these marine natural products have antitumor effects. Bryostatins are currently in phase II clinical trials and show promise as anticancer drugs, particularly when combined with other adjuvant therapy. 

PTKs have been implicated in the regulation of a variety of biological responses such as cell proliferation, migration, differentiation, and survival. They have been demonstrated to play significant roles in the development of many disease states, including immunodeficiency, atherosclerosis, psoriasis, osteoporosis, diabetes, and cancer. In recent clinical trials impressive antitumor effects of PTK inhibitors have been observed. In future, PTK inhibitors may therefore become important drugs for the treatment of specific cancers. 

Kroes, R.A., Abravaya, K., Seidenfeld, J., Morimoto, R.l. (1991). Selective activation of human heat shock gene transcription by nitrosurea antitumor drugs mediated by isocyanate-induced damage and activation of heat shock transcription factor. Proc. Natl. Acad. Sci. USA 88,4825-4829. 

The platinum complex (NH3)2PtCl2 is a well-known antitumor agent. Because the drug is soluble in water, it is readily excreted through the kidneys and can cause severe kidney damage. Various procedures are employed clinically to minimize these side effects, but the... 

Prior to the study by Chen et al. (140), only one publication discussed the use of the protein casein as a drug carrier (141). Chen et al. systematically compared the many features of albumin and casein microspheres—morphology, drug (adriamycin) incorporation, and release—in an effort to identify important factors in the antitumor effect of this delivery system. 

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