As antineoplastic agents

The epidermal growth factor receptor 2 (HER-2) is a protein found on the surface of cells. Heterodimerization of HER-2 activates the enzyme tyrosine kinase, triggering reactions that cause the cells to grow and multiply. HER-2 is found at abnormally high levels on the surface of many types of cancer cells, which may divide excessively. Antibodies targeting HER-2 (e.g., trastuzumab) are used as antineoplastic agents. 

Examples of acridin alkaloids used in therapeutics as antineoplastic agents is amsacrine (Amsa P-D ), which is used for the treatment of acute leukemia in adults and malignant lymphomas, refractory to conventional therapy. Amsacrin is an intercalating agent and topoisomerase II inhibitor. 

Gao L, Cueto MA, Asselbergs F, Ataoja P (2002) Cloning and functional characterization of HDACll A novel member of the human histone deacetylase family. J Biol Chem 277 25748-25755 Garcia-Manero G, Issa JP (2005) Histone deacetylase inhibitors A review of their clinical stams as antineoplastic agents. Cancer Invest 23 635-642... 

Finally these compounds may also present in the future some interest in the area of novel anti-tumor drugs, or in photochemotherapy [12], Up to now the mechanism of action of the Pt complexes as antineoplastic agents has been extensively examined [13]. In spite of their successful applications, there is a need in compounds that are less toxic than the Pt derivatives. Therefore novel photo-active metallic compounds could offer future possibilities for cancer treatment. The fact that a drug would become active exclusively under illumination might represent an advantage. 

The binary indole-indoline alkaloids vinblastine (VLB, 1) and vincristine (VCR, 2) (Fig. 1) have triggered considerable chemical investigation as a result of their extensive clinical use as antineoplastic agents (2-4), coupled with an arduous isolation from plant material, and because of... 

Diazoazoles find wide application in the preparation of azolo-triazenes, which have shown several biological activities expecially as antineoplastic agents. Triazenes are, in effect, latent diazo compounds because they decompose to give amino derivatives and diazonium salts so they can be employed as a carrier group for the diazo compounds (66JMC34). 

Platinum complexes (e.g., di-platinum, 8.100) are used as antineoplastic agents in the treatment of cancer. Their use is described in chapter 7. 

As well as their chemical importance, appropriate oxy-1,6-naphthyridines have shown appreciable (but not outstanding) biological activities as metal-binding antibacterials,110 or as antineoplastic agents.572,cf 843 Medorinone, 5-methyl-1,6-naphthyridin-2(lH)-one, has been used as a cardiotonic/vasodilatory agent.490, 716,1224,cf. 320 QXy derivatives of fused/unfused 1,6-naphthyridines have been iso-lated from manne sponges. ... 

Chloroethyl)phosphorodiamidate mustards, (VII), prepared by Herr (7) were effective as antineoplastic agents especially in the treatment of solid tumors. 

Vm. Cervical Cancer Immune Response Modifiers as Antineoplastic Agents... 

Garcia-Manero G, Issa JP. Histone deacetylase inhibitors a review of their clinical status as antineoplastic agents. Cancer 109. Invest. 2005 23 635-642. 

Inhibitors of pyrimidine and purine biosynthesis are used as antineoplastic agents. As a consequence, dihydroorotase, which catalyzes the third step of de novo pyrimidine biosynthesis, the conversion of carbamyl aspartate to dihydroorotate (Equation 17.43), is a target for therapeutic intervention. 

Vinca alkaloids (vincristine, vinblastine, vinorelbine) are derived from the periwinkle plant (Vinca rosea). These agents work by binding to tubulin at a site different than colchicine or paclitaxel. They block polymerization, which prevents the formation of the mitotic spindle, and are used as antineoplastic agents. Taxanes produce a stabilization of microtubules similar to colchicine, but by a different mechanism, and also halt cells in metaphase. Paclitaxel (taxol) is the taxane used clinically. It is derived from the bark of the pacific yew. Taxol disrupts several microtubule-based functions as completely as inhibitors of polymerization, emphasizing the importance of assembly/disassembly balance in microtubule function. Recently, it has been found that paclitaxel also binds to and inhibits the function of a protein called bcl-2, an inhibitor of one or more pathways involved in mediating apoptosis. PaclitaxeTs interference with this function promotes apoptosis in addition to its microtubule-related inhibition of cell division. 

Metal containing compounds are attracting increasing attention as antineoplastic agents Cisplatin is established as useful therapy for treatment of testicular and ovarian tumors, although associated severe side effects limit the doses that may be given to patients Work is underway to develop less toxic, equally efficacious agents... 

Daunorubicin, doxorubicin, epirubicin, and idarubicin are examples of anthracycline antibiotic agents. These agents are used as antineoplastic agents. 

List the two major vinca alkaloids used as antineoplastic agents. 

A few important nitrogen mustards used as antineoplastic agents are discussed below, for instance Mechlorethamine hydrochloride, Mephalan, Cyclophosphamide and Chlorambucil. 

What is a neoplasm What are the causations of neoplasm Give the structure, name and uses of at least three potent dmgs employed as antineoplastic agents belonging to ... 

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