+ Site Statistics
References:
54,258,434
Abstracts:
29,560,870
PMIDs:
28,072,757
+ 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 chemistry and biology of new generation taxoids



Recent advances in the chemistry and biology of new generation taxoids



Journal of Natural Products 72(3): 554-565



Among the numerous chemotherapeutic drugs, paclitaxel and docetaxel are among the most widely used against various types of cancer. However, these drugs cause undesirable side effects as well as drug resistance. Therefore, it is essential to develop "taxane" anticancer agents with better pharmacological properties and improved activity especially against drug-resistant cancers. Several laboratories have performed extensive SAR studies on paclitaxel. Our SAR studies have led to the development of numerous highly potent novel second- and third-generation taxoids with systematic modifications at the C-2, C-10, and C-3' positions. The third-generation taxoids showed virtually no difference in potency against drug-resistant and drug-sensitive cell lines. Some of the new generation taxoids also exhibited excellent cytotoxicity against pancreatic cell lines expressing multidrug-resistant genes. We have also designed taxoids with strategic fluorine incorporation to investigate their effects on the cytotoxicity and the blockage of known metabolic pathways. Furthermore, we have successfully employed computational biology analysis to design novel macrocyclic taxoids to mimic the bioactive conformation of paclitaxel. This account describes our work on the design, synthesis, and biological evaluation of these novel taxoids, which has led to the discovery of very promising candidates for further preclinical studies.

(PDF emailed within 0-6 h: $19.90)

Accession: 055398805

Download citation: RISBibTeXText

PMID: 19239240

DOI: 10.1021/np8006556


Related references

Recent Advances in the Chemistry and Biology of New Generation Taxoidsa¬°. 2009

Recent advances in the medicinal chemistry of taxoids with novel beta-amino acid side chains. Current Medicinal Chemistry 6(10): 927-954, 1999

Recent advances in chemistry and biology of gamboge. Zhongguo Zhong Yao Za Zhi 38(1): 19-25, 2013

Recent advances in the biology and chemistry of the flavaglines. Bioorganic & Medicinal Chemistry 20(6): 1857-1864, 2012

Recent advances in the chemistry and biology of penicillins. Brown, A G And S M Roberts (Ed ) Royal Society Of Chemistry Special Publication, No 52 Recent Advances in The Chemistry Of B-Lactam Antibiotics; 3rd International Symposium, Cambridge, England, July 2-4, 1984 Viii+391p The Royal Society Of Chemistry: London, England Illus Paper 32-51, 1985

Recent advances in the chemistry and biology of sea water. Recent advances in the chemistry and biology of sea water vii+164p 29 fig, 1945

Recent Advances in the Chemistry and Biology of Podophyllotoxins. Chemistry (): -, 2016

Recent advances in the chemistry and biology of benzothiazoles. Archiv der Pharmazie 348(3): 155-178, 2015

Recent advances in the chemistry & biology of sea water. 1945

Recent advances in the biology and chemistry of vitamin D. Fortschritte der Chemie Organischer Naturstoffe 39: 63-121, 1980

Recent advances in the chemistry and biology of pyridopyrimidines. European Journal of Medicinal Chemistry 95: 76-95, 2016

Recent advances in L-nucleosides: chemistry and biology. Antiviral Research 40(1-2): 19-44, 1998

Recent advances in the chemistry and biology of retinoids. Progress in Medicinal Chemistry 30: 1-55, 1993

Recent advances in the chemistry and biology of antimycobacterial agents. Bristol, J A Annual Reports in Medicinal Chemistry: 161-170, 1996

Recent advances in liver X receptor biology and chemistry. Current Topics in Medicinal Chemistry 8(9): 781-791, 2008