[PDF][PDF] Tubulin and microtubules as targets for anticancer drugs

JA Hadfield, S Ducki, N Hirst… - Progress in Cell Cycle …, 2003 - researchgate.net
The vinca alkaloids have been used in the treatment of cancer for over 40 years. Their
efficacy has ensured that they remain among the drugs of choice for a number of human …

Chemistry and chemical biology of taxane anticancer agents

ML Miller, I Ojima - The Chemical Record, 2001 - Wiley Online Library
Taxol®(paclitaxel) and Taxotère®(docetaxel) are currently considered to be among the most
important anticancer drugs in cancer chemotherapy. The anticancer activity of these drugs is …

BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy

FYF Lee, R Borzilleri, CR Fairchild, SH Kim… - Clinical Cancer …, 2001 - AACR
BMS-247550, a novel epothilone derivative, is being developed by Bristol-Myers Squibb
Company (BMS) as an anticancer agent for the treatment of patients with malignant tumors …

The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions …

RJ Kowalski, P Giannakakou, SP Gunasekera… - Molecular …, 1997 - ASPET
The lactone-bearing polyhydroxylated alkatetraene (+)-discodermolide, which was isolated
from the sponge Discodermia dissoluta, induces the polymerization of purified tubulin with …

A common pharmacophore for cytotoxic natural products that stabilize microtubules

I Ojima, S Chakravarty, T Inoue, S Lin… - Proceedings of the …, 1999 - National Acad Sciences
Taxol (paclitaxel), a complex diterpene obtained from the Pacific yew, Taxus brevifolia, is
arguably the most important new drug in cancer chemotherapy. The mechanism of cytotoxic …

Quest for efficacious next-generation taxoid anticancer agents and their tumor-targeted delivery

I Ojima, X Wang, Y Jing, C Wang - Journal of natural products, 2018 - ACS Publications
Paclitaxel and docetaxel are among the most widely used chemotherapeutic drugs against
various types of cancer. However, these drugs cause undesirable side effects as well as …

On the remarkable antitumor properties of fludelone: how we got there

A Rivkin, TC Chou… - Angewandte Chemie …, 2005 - Wiley Online Library
Small‐molecule natural products are presumably often biosynthesized with a view to
optimizing their ability to bind to strategic proteins or other biomolecular targets. Although …

Highly concise routes to epothilones: The total synthesis and evaluation of epothilone 490

K Biswas, H Lin, JT Njardarson… - Journal of the …, 2002 - ACS Publications
A concise modular laboratory construction of the epothilone class of promising antitumor
agents has been accomplished. For the first time in the epothilone area, the new synthesis …

Discovery of (E)-9,10-Dehydroepothilones through Chemical Synthesis:  On the Emergence of 26-Trifluoro-(E)-9,10-dehydro-12,13-desoxyepothilone B as a …

A Rivkin, F Yoshimura, AE Gabarda… - Journal of the …, 2004 - ACS Publications
We provide a full account of the discovery of the (E)-9, 10-dehydro derivatives of 12, 13-
desoxyepothilone B (dEpoB), a new class of antitumor agents with promising in vivo …

A Total Synthesis of Epothilones Using Solid‐Supported Reagents and Scavengers

RI Storer, T Takemoto, PS Jackson… - Angewandte Chemie …, 2003 - Wiley Online Library
The epothilone natural products [1] exhibit extraordinary cytotoxic biological activity by
promoting GTP-independent tubulin polymerization. This mode of action inhibits the growth …