Neoplastic agents

Lee FYF, Borzilleri R, Fairchild CR, Kamath A, Smykla R, Kramer R, Vite G. (2008) PrecUnical discovery of ixabepilone, a highly active anti-neoplastic agent. Cancer Chemother Pharmacol 63 157-166. 

Camptothecin (Fig. 4), a quinoline alkaloid, is a potent anti-neoplastic agent that inhibits DNA topoisomerase I. Accumulation of up to 8 mg of camptothecin/L was reported for hairy root cultures of Ophiorriza pumila transformed with A. rhizogenes. Cotyledon-derived calluses of Nothapodytes foetida were able to produce not only camptothecin, but also its derivatives also known to exhibit anticancer activity. 

Anti-neoplastic agents and immunosuppressants Anti-protozoal agents Anti-thyroid agents... 

Figure 7.5 Intercalation of carcinogens into the stacked bases of nucleic acids. Both carcinogens and certain anti-neoplastic agents share a common mechanism of action. They have the capacity to insert themselves into the nucleic acid structure, causing geometrical distortions that preclnde the ability of the nucleic acid to complete its function in the processes of transcription and translation. Flat aromatic molecules have the ability to intercalate between the stacked bases.

Antimetabolite The general term for drugs that impair function in harmful cells and microorganisms by antagonizing or replacing normal metabolic substrates in those cells. Certain anti-infectious and anti-neoplastic agents function as antimetabolites. 

L, M, Botana, E. Ameer, M. R. Vieytes, el al. Ncm-immunological release of histamine fiom rat mast cells elicited by anti neoplastic agents. Cancer Chanother. 

Besides their utilization in the production of many compounds with therapeutic, diagnostic, and immunizing applications, animal cell cultures have undoubted utility in the performance of in vitro cytotoxicity tests. They can be used for the evaluation of potential anti-neoplastic agents and assessment of the safety of various products, such as pharmaceuticals, cosmetics, alimentary additives, pesticides, and industrial chemical products. Cell culture systems are frequently employed in the cancer chemotherapy field, in which their potential value for viability and cytotoxicity tests is largely accepted. Animal models play an important role in toxicity testing, but the pressure to adopt in vitro tests is growing since they present considerable economical advantages over in vivo tests. The use of animal models is limited to human metabolism studies, and there are... 

Many 6-alkylaminopurine nucleosides are important adenosine receptor antagonists, and acyclic nucleotide analogues derived from 6-dialkylaminopurines are strong antivirals, anti-neoplastic agents, and immunomodulators. Recently, several 6-(arylalkynyl)-, 6-(arylalkenyl)-, and 6-(arylalkyl)purines have been reported to exhibit cytokinine activity. Suzuki crosscoupling reactions of 9-benzyl-6-chloropurine with boronic acids have recently been reported to provide 6-substituted purines in moderate to excellent yields (Eq. (46)) [77]. 

Milk fat contains small amounts of ether lipids. Synthetic ether lipids at low concentrations are potent anti-neoplastic agents. Cell culture studies showed that they inhibited cell growth, induced differentiation, promoted apoptosis and showed anti-metastatic activity. In human chemoprevention trials ether lipids have been administered parenterally. Although the ether bond is preserved when these lipids are delivered orally, no cancer chemoprevention studies have utilized dietary ether lipids (Parodi, 2004). 

Related applications include peptide/protein hydrolysis, heterogeneous catalysis reactions, acid digestion of samples, (e.g. tissue, implants, catalysts, drugs, etc), for AA / ICP / ICP-MS analysis, solvent extractions, processing and/or destruction of toxic chemicals, chemotherapy and anti-neoplastic agents. 

A large number of plant-derived compounds are apoptotic., having been variously shown to activate caspases, cause membrane blebbing or induce formation of a ladder of fragmented DNA. Such compounds are cytotoxic and have potential as anti-neoplastic agents (Table 9.7). 

S.M. Kerwin etal, US Patent 6,297,284 (October 2, 2001) Assignee Research Development Foundation Utility Anti-Neoplastic Agent... 

Aza-enediynes are a new class of anti-neoplastic agents that produce a cytotoxic effect through an aza-Bergman cyclization (1) of an enediyne core to a 1,4-didehydrobenzene reaction intermediate. Both Bergman and benzothiazolium salt diradical cyclizations are illustrated in Eq. 1 and Eq. 2, respectively. 

R.F. Borch etal, US Patent 6,656,926 (December 2, 2003) Assignee Purdue Research Foundation Utility Anti-Neoplastic Agent for Animals... 

S.G. Dimagno, US Patent 6,392,032 (May 21, 2002) Assignee Board of Regents University of Nebraska-Lincoln Utility Anti-Neoplastic Agents... 

Utility Anti-Neoplastic Agent Inhibitor of DNA Replication... 

C.T. Chang etaU US Patent 6,046,229 (April 4, 2000) Assignee Industrial Technology Research Institute Utility Anti-Neoplastic Agents for Inoperable or Metastatic Cancers... 

Fox, C.H., and Eberl, M., 2002, Phytic acid (IP6), novel broad spectrum anti-neoplastic agent A systematic review. Complement. Ther. Med. 10 229-234. 

Thus, the mucolytic agent iV-acetyl-L-cys-teine is predicted to have a potential to induce allergic contact dermatitis by virtue of the biophore SH—CHg (Fig. 19.5). Moreover, examination of the chemicals that contribute to that toxicophore reveals that indeed they all have the substructure in an environment that is similar to the one found inN-acetyl-L-cysteine (Table 19.3). On the other hand, the tubulin polymerization perturber (and potential anti-neoplastic agent) epitholone A (Fig. 19.6) is predicted to be a mouse carcinogen by virtue of the toxicophore units shown in bold. That toxicophore is present in five molecules in the learning set. The presence of that toxicophore... 

Safirstein RL Renal disease induced by anti-neoplastic agents., chap. 43, in Diseases of the Kidney and Urinary Tract., 8th ed., edited by Schrier RW, Philadelphia, Lippincott, Williams and Wilkins, 2007, pp 1068-1081 Andrade L, Vieira JM, Safirstein R How Cells Die Counts. Am J Kidney Dis. 36 662-668, 2000... 

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