โ Scribed by Gunda I. Georg; Thomas C. Boge; Haeil Park; Richard H. Himes
No coin nor oath required. For personal study only.
The synthesis and in vitro evaluation of four novel 3-azidobenxoyl photoaffinity analogues of paclltaxel and docetaxel is detailed. Due to their good to excellent ability to stimulate the assembly of microtubules they have potential as photo&finity probes.
๐ SIMILAR VOLUMES
Radiolabeled paclitaxel and three photophore-bearing derivatives were prepared by organoiridiummediated direct tritium exchange under both catalytic and stoichiometric conditions. The resulting tritiated taxoids had specific activities ranging from 53 to 195 Ci/mmol.
## Abstract Tumor growth requires a competent vascular supply and angiogenesis has been considered as a potential target for the treatment of several cancers. The two clinically approved taxanes, paclitaxel and docetaxel, are novel antimitotic agents that are under extensive investigation in clinic
A useful method for preparing radioiodinated photoaffinity labels from alkyl anilines which offers significant advantages over present methods is described. The one-pot synthesis gives good radiochemical yields (40-64%) of pure, high specific activity (350 -1500 mCi/pmol) 1251 labelled iodoatyl azid