By Iwao Ojima, Gregory D. Vite, Karl-Heinz Altmann
Melanoma drug discovery and improvement : new paradigms for a brand new millennium / E.A. Sausville ... [et al.] --
Evolutionary biosynthesis of anticancer medicinal drugs / George R. Pettit --
Some contemporary advancements within the synthesis and structure-activity courting 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 mix in human carcinoma cellphone strains / Susan Band Horwitz ... [et al.] --
Highly effective semisynthesis of biologically energetic epothilone derivatives / Gregory D. Vite ... [et al.] --
Synthetic and semisynthetic analogs of epothilones : chemistry and organic task / 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 --
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Farnesyltransferase inhibitors as strength anticancer brokers / J.B. Gibbs ... [et al.] --
Farnesyltransferase inhibitors : from squalene synthase inhibitors to the scientific agent BMS-214662 / John T. Hunt --
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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 discovery and improvement of second-generation matrix metalloproteinase inhibitors for the therapy of melanoma / Andy Baxter and John Montana --
Prospects for antiangiogenic treatments 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 --
Drugs 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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Extra info for Anticancer agents : frontiers in cancer chemotherapy
Zhuang, L . Tetrahedron Lett. 1997, 38, 8675-8678. Pettit, G . ; Cichacz, Ζ. ; Herald, C . ; Boyd, M. R. J. Chem. Soc, Chem. Commun. 1993, 14, 1166-1168. Pettit, G . ; Herald, C . ; Cichacz, Ζ. ; Schmidt, J. ; Boyd, M. ; Christie, N. D . ; Boettner, F . E . J. Chem. Soc. Chem. Commun. 1993, 1805-1807. Pettit, G . ; Herald, C . ; Cichacz, Ζ. ; Gao, F . ; Boyd, M. ; Christie, N. D . ; Schmidt, J. M. Nat. Prod. Lett. 1993, 3, 239-244. Pettit, G . ; Cichacz, Ζ. ; Herald, C . ; Gao, F . ; Boyd, M.
Thus we relied on our knowledge of the highfield NMR characteristics of the components to direct the total synthetic approaches. Each of the total syntheses we completed required about 28 steps; they were not easy at the beginning and it took 15 total syntheses (114,115) to prepare the natural product, a definite improvement over the theoretical 512! Subsequently, we prepared dolastatin 10 for clinical trials by total synthesis, and NCI phase II cancer clinical trials are under way. Current results indicate, for example, a good future in the treatment of refractory A M L .
MDR resistant human colon tumor cell line. Ratio of I C for HCT 116(VM)46 MDR resistant cell line /IC for HCT 116 sensitive cell line. Paclitaxel sensitive human ovarian tumor cell line. ^Paclitaxel resistant human ovarian tumor cell line known to be resistant due to a β-tubulin mutation (T. Fojo, NCI(23)). g Ratio of I C for human ovarian resistant cell line /IC for A2780 senstive cell line. b C d 50 50 e 50 50 against an ip/ip M109 tumor model(16). This initial in vivo screen minimizes the impact of pharmokinetics since both the tumor and drug are placed in the intraperitoneal cavity and provides initial indications of activity and potency.