Cancer agents

Despite dramatic advances in the treatment of several human malignancies including Hodgkin s lymphomas and leukemias, dmg resistance remains a pressing issue in cancer chemotherapy. Acquired or induced dmg resistance afflicts practically all classes of cancer agents. It usually is manifested clinically... 

The recent links made between mTORCl and tumor suppressors/oncoproteins suggests that aberrantly high mTORCl activity may be the underlying cause of hamartomas and perhaps some cancers. Based on this, many clinical trials are underway to determine the efficacy of rapalogs as anti-cancer agents. Current phase III clinical trials include ... 

However, an almost classical attempt to generate an a, -unsaturated e-capro-lactam 87 involved a Knoevenagel condensation of 86 as the ring forming step. The material was employed in a synthesis of conformationally restricted analogs of some anti cancer agents (tetrahydrofolate analog) (Scheme 17) [24]. 

Baldwin R.W. (1985) Monoclonal antibody targeting of anti-cancer agents. EurJ Cancer Clin Oncol, 21, 1281-1285. 

Sordet O, Khan QA, Konh KW, Pommier Y (2003) Cmr Med Chem Anti-Cancer Agents 3 271... 

A second highly soluble diphosphate derivate, 3.17, was also produced (solubility 29mg/mL) its efficacy in an in vitro cancer agent was screened, and it proved to be the most active carotenoid ever tested in this system (Hix et al. 2005), and more potent than Cardax, 3.19 (Hix et al. 2004). Overall, the second-generation compounds showed increased promise over the prototypes in certain contexts, particularly those in which immediate radical scavenging by highly potent and soluble compounds are required. 

Another anti-cancer agent in clinical use is podophyllotoxin (3-59) this has an aryl tetrahydronaphthalene lignan lactone skeleton, and demonstrates potent tubulin-binding, anti-mitotic properties (Scheme 3.16) [30]. The Sherburn group [31] prepared this molecule by a tris(trimethylsilyl)silane promoted conversion of thionocarbonate 3-55 into the lactone 3-58, which proceeded with a yield of 38 %. As intermediates, the radicals 3-56 and 3-57 can be assumed. 

M. P. Edwards, Discovery of cMet Kinase Inhibitors as Potential Anti-Cancer Agents, 11th Annual San Diego Med. Chem. Symposium, UCSD, California, July, 2008. 

Quinoxaline bis-A-oxides have been investigated as potential anti-cancer agents 93 <06BMC6917> and anti-trypanosomal agents 94 <06BMC5503>. In the latter case, a vanadyl complex was prepared in order to increase bioavailability. 

The answer is c. (Hardman, pp 1260—1262.) Paclitaxel is a large structural molecule that contains a 15 membered taxane ring system. This anti cancer agent is an alkaloid derived from the bark of the Pacific yew tree. Its chemotherapeutic action is related to the microtubules in the cell. Paclitaxel promotes microtubule assembly from dimers and causes microtubule stabilization by preventing depolymerization. As a consequence of these actions, the microtubules form disorganized bundles, which decreases... 

The immunostimulatory activity of IL-2 has proven beneficial in the treatment of some cancer types. An effective anti-cancer agent would prove not only medically valuable, but also commercially very successful. In the developed world, an average of one-in-six deaths is caused by cancer. In the USA alone, the annual death toll from cancer stands in the region of half a million people. 

The initial interest in utilizing TNF as a general anti-cancer agent has diminished, largely due to the realization that ... 

Thrombolytic agent Thrombolytic agent Anticoagulant Haemophilia B Anti-cancer agent Cystic fibrosis Gaucher s disease Fabry disease Hyperuricaemia Mucopolysaccharidosis Oxygen toxicity Pompe disease... 

De Medina P, Favre G, Poirot M (2004a) Multiple targeting by the antitumor drug tamoxifen a structure-activity study. Curr Med Chem Anti-Cancer Agents 4(6) 491-508... 

Wiseman H, Cannon M, Arnstein HR, Barlow DJ (1992a) The structural mimicry of membrane sterols by tamoxifen evidence from cholesterol coefficients and molecular-modelling for its action as a membrane anti-oxidant and an anti-cancer agent. Biochim Biophys Acta 1138(3) 197-202... 

Catharanthus roseus) [9]. Maytansine (3) is an ansa macrolyde isolated from Maytenus ovatus [10], and rhizoxin (4) is an antitumor macrolide isolated from the fungus Rhizopus chinensis [11]. Another very important tubulin interactive anti-cancer agent is colchicine (6), and this compound binds to a different binding site of tubulin but is also used in anti-cancer therapy. 

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