Antimicrotubule Agents

The synthesis of a range of analogues and derivatives allowed a structure-activity relationship to be deduced for paclitaxel, informing the semi-synthesis of other taxanes for biological evaluation

2017

Scholarcy highlights

  • The synthesis of a range of analogues and derivatives allowed a structure-activity relationship to be deduced for paclitaxel, informing the semi-synthesis of other taxanes for biological evaluation
  • Paclitaxel had been demonstrated to be a potent anticancer agent, the problems associated with obtaining sufficient quantities threatened to halt its development until it was discovered that, in addition to having a novel structure, it had a unique mode of action
  • Myelosuppression is considered the principal toxicity associated with the taxanes: it is more commonly associated with docetaxel, and occurs with paclitaxel and cabazitaxel
  • The vinca alkaloids are antimicrotuble agents used in the treatment of a range of cancers, including; breast, bladder, kidney, testicular, and lung cancers, leukaemias, lymphomas, melanoma, and myeloma
  • Common adverse effects associated with the vinca alkaloids include fatigue, peripheral neuropathy, constipation, diarrhoea, myelosuppression, and loss of fertility

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