+ Site Statistics
+ Search Articles
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ PDF Full Text
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Translate
+ Recently Requested

Recent advances in the new generation taxane anticancer agents

Recent advances in the new generation taxane anticancer agents

Medicinal Chemistry ) 1(2): 125-139

Recent advances in the design and preclinical evaluations of promising new generation taxane anticancer agents are reviewed in this article. Paclitaxel and docetaxel are two of the most important anticancer drugs today. However, recent reports have shown that treatment with these drugs often encounters undesirable side effects as well as drug resistance. Therefore, it is important to develop new taxane anticancer agents with fewer side effects, superior pharmacological properties, and improved activity against drug-resistant human cancers. Structure-activity relationship (SAR) studies led to the discovery of a series of highly active second-generation taxanes. One of them, "Ortataxel" (SB-T-101131, IDN5109, BAY59-8862), exhibits excellent activity against a variety of drug-sensitive and drug-resistant cancer cell lines, as well as human tumor xenografts in mice. It is orally active and is currently in phase II clinical trials. Photoaffinity labeling of microtubules and P-glycoprotein using photoreactive radiolabeled taxoids has disclosed the drug-binding domain of tubulin as well as Pgp. Together with information on microtubule-bound fluorine-labeled taxoids obtained by solid-state NMR studies, the bioactive conformation of paclitaxel and taxoids appears to emerge. Novel taxane-monoclonal antibody (mAb) immunoconjugates, have shown highly promising results for the tumor-specific delivery and release of an extremely cytotoxic, second-generation taxane. Also, another novel series of second generation taxanes conjugated with n-3 polyunsaturated fatty acids, e.g. decosahexaenoic acid (DHA), has exhibited impressive antitumor activity with minimum general toxicity against the highly drug-resistant DLD-1 human colon cancer xenografts in SCID mice.

(PDF emailed within 1 workday: $29.90)

Accession: 050126376

Download citation: RISBibTeXText

PMID: 16787308

Related references

Discovery, development, and chemical biology of new generation taxane anticancer agents. Abstracts of Papers American Chemical Society 221(1-2): ORGN 200, 2001

Overview: Recent Advances in Antifolates as Anticancer Agents. Expert Opinion on Therapeutic Patents 2(12): 1979-1992, 1992

Recent Advances in Development of Polyphenols as Anticancer Agents. Mini Reviews in Medicinal Chemistry 18(15): 1265-1269, 2018

Recent Advances in Copper Intercalators as Anticancer Agents. Journal of Fluorescence 28(5): 1195-1205, 2018

Recent Advances in the Development of Indazole-based Anticancer Agents. Chemmedchem 13(15): 1490-1507, 2018

Transition Metal Intercalators as Anticancer Agents-Recent Advances. International Journal of Molecular Sciences 17(11), 2016

Recent Advances of Natural and Synthetic β-Carbolines as Anticancer Agents. Anti-Cancer Agents in Medicinal Chemistry 15(5): 537-547, 2016

Recent advances in oral anticancer agents for colon cancer. Future Oncology 9(12): 1893-1908, 2014

Novel anticancer agents and targets: recent advances and future perspectives. Mini Reviews in Medicinal Chemistry 13(9): 1239-1255, 2014

Recent Advances in the Development of Thioredoxin Reductase Inhibitors as Anticancer Agents. Current Drug Targets 13(11): 1432-1444, 2012

Recent advances in pharmacologic study of natural anticancer agents in China. Memorias do Instituto Oswaldo Cruz 86 Suppl 2: 51-54, 1991

Recent advances in the development of thioredoxin reductase inhibitors as anticancer agents. Current Drug Targets 13(11): 1432-1444, 2013

Recent Advances in Multinuclear Complexes as Potential Anticancer and Dna Binding Agents. Anti-Cancer Agents in Medicinal Chemistry 14(1): 147-169, 2014

Recent advances in multinuclear complexes as potential anticancer and DNA binding agents. Anti-Cancer Agents in Medicinal Chemistry 14(1): 147-169, 2014

Recent advances in drug discovery of phototherapeutic non-porphyrinic anticancer agents. European Journal of Medicinal Chemistry 142: 459-485, 2017