Studies On Combretastatin A-4 Targeting Conjugates

Combretastatin A-4(CA-4),as a drug which has antitumor ability,was getting more and more concerned in recent years.However,the poor water solubility,low bioavailability and toxicity to normal cells brought down the quantities of reports on CA-4 druggability solely.To avoid the drawbacks of the entity CA-4,numerous researchers on medicinal chemistry designed various CA-4 conjugates.These conjugates have special abilities,such as high water solubility,safe to normal cells or target delivering,and had achieved relatively fruitful results.In this article,we reviewed all sort of the achievements on the research of CA-4 conjugates from five decades before to present,and to evaluate the real sense of all the inventions.We emphasize our work on a series of the targeting CA-4 conjugates,which were referred to the researchers' work.Our targeting CA-4 conjugates contain a quinone propionic acid(QPA)moiety,the structure QPA could self-cycling once it was hydrolyzed by NAD(P)H dehydrogenase [quinone] 1(NQO1)and NAD(P)H,thus specially delivering CA-4 into cancer cells.The design of novel CA-4 conjugates might solve the problem that the parent drug CA-4 itself have no selectivity to cancer cells.