By Iwao Ojima, Gregory D. Vite, Karl-Heinz Altmann

content material: melanoma drug discovery and improvement : new paradigms for a brand new millennium / E.A. Sausville ... [et al.] --
Evolutionary biosynthesis of anticancer medicines / George R. Pettit --
a few fresh advancements within the synthesis and structure-activity dating of novel taxanes / John F. Kadow ... [et al.] --
New new release taxoids and hybrids of microtubule-stabilizing anticancer brokers / Iwao Ojima ... [et al.] --
Discodermolide and taxol : a synergistic drug mixture in human carcinoma mobile traces / Susan Band Horwitz ... [et al.] --
hugely effective semisynthesis of biologically energetic epothilone derivatives / Gregory D. Vite ... [et al.] --
artificial and semisynthetic analogs of epothilones : chemistry and organic job / Karl-Heinz Altmann ... [et al.] --
Synthesis and organic task of epothilones / Ulrich Klar ... [et al.] --
Epothilones and sarcodictyins : from combinatorial libraries to designed analogs / Nicolas Winssinger and K.C. Nicolaou --
Synthesis and structure-activity dating reviews of cryptophycins : a unique category of effective antimitotic antitumor depsipeptides / Chuan Shih ... [et al.] --
Farnesyltransferase inhibitors as capability anticancer brokers / J.B. Gibbs ... [et al.] --
Farnesyltransferase inhibitors : from squalene synthase inhibitors to the medical agent BMS-214662 / John T. Hunt --
Inhibiting farnesyl protein transferase with Sch-66336 : most likely a selective noncytotoxic treatment for human melanoma / A.G. Taveras ... [et al.] --
Pyrrolo[2,3-d]pyrimidine and pyrazolo[3,4-d]pyrimidine derivatives as selective inhibitors of the EGF receptor tryosine kinase / G. Caravatti ... [et al.] --
STI571 : a brand new therapy modality for CML? / Jürg Zimmermann, Pascal Furet, and Elisabeth Buchdunger --
the invention and improvement of second-generation matrix metalloproteinase inhibitors for the therapy of melanoma / Andy Baxter and John Montana --
clients for antiangiogenic remedies established upon VEGF inhibition / Pascal Furet and Paul W. Manley --
Carbohydrate-based tumor antigens as antitumor vaccine brokers / Jennifer R. Allen and Samuel J. Danishefsky --
medications to augment the healing efficiency of anticancer antibodies : antibody-drug conjugates as tumor-activated prodrugs / Walter A. Blättler and Ravi V.J. Chari.

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D . ; Croom, D . ; Emerson, D . ; Evans, M . G . ; Leitner, P. ; Luzzio, M. J . ; Mclntyre, G . ; Besterman, J. M. J. Med. Chem. 1996, 39, 713-719. ; Pinedo, H. Camptothecins: New Anticancer Agents; C R C Press: F L , 1995. Ojima, I. Adv. Med. Chem. 1999, 4, 69-124. Gunatilaka, Α. ; Ramdayal, F . D . ; Sarragiotto, M. ; Kingston, D . G . I. Sackett, D . ; Hamel, E . J. Org. Chem. 1999, 64, 2694-2703. Jagtap, P. G . ; Kingston, D . G . I. Tetrahedron Lett. 1999, 40, 189-192. ; Kuwajima, I. J. Am.

I. J. Nat. Prod. 2000, 63, 457-460. Pettit, G . ; Cragg, G . ; Gust, D . ; Brown, P . ; Schmidt, J . M. Can. J. Chem. 1982, 60, 939-941. Pettit, G . ; Cragg, G . ; Brown, P. Can. J. Chem. 1982, 60, 544-546. Pettit, G . ; Cragg, G . ; Niven, M. ; Nassimbeni, L. R. Can. J. Chem. 1983, 61, 2630-2632. Pettit, G . ; Cragg, G . ; Suffness, M. ; Boettner, F . ; Saenz-Renauld, J . Α . ; Brown, P . ; Schmidt, J. ; Ellis, P. D . J. Org. Chem. 1984, 49, 4258-4266. Pettit, G . R . ; Cragg, G . ; Suffness, M.

Values are %T/C analog ( maximum tolerated dose) / % T/C for paclitaxel (200 to 259)at a historically determined efficacious dose but does not represent the MTD. %T/C values of > 125 % are considered active. 50 50 c 50 BMS 184476, The 7-MTM analog of paclitaxel. The parent M T M compound, 15, which showed a significant but more moderate ability to overcome resistance, was also evaluated in distal tumor models. ; ACS Symposium Series; American Chemical Society: Washington, DC, 2001. 51 was found to be highly active and curative in some moderately staged tumor models.

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