Review of Cytotoxic CA4 Analogues that Do Not Target Microtubules: Implications for CA4 Development.

BACKGROUND: One of the most studied anti-cancer compounds of the last several decades is the microtubule targeting agent and cis-stilbene, combretastatin A4 (CA4). Despite promising results at the pre-clinical level, future clinical use of CA4 as a monotherapy is in question due to metabolic vulnerability and conformational instability. OBJECTIVE: Thus, medicinal chemists have focused on synthesizing derivatives with improved pharmokinetic …