Ene Synthesis Study Of The Diyne Unit. Ene-diyne Antitumor Antibiotic

Natural enediyne antibiotics(e.g. Neocarzinostatin, Kedarcidin, Maduropeptin, C-1027, Calicheamicins, Dynemicins, Esperamicins) are among the most powerful antitumoral compounds known to date. The most interesting feature of these compounds is that they are natural prodrugs: their biological activity is indeed "triggered" by a particular transformation, which unleashes the reactivity of the enediyne moiety leading,upon Bergman cycloaromatizayion, to highly reactivity aromatic diradicals. Researches from a number of disciplines have been devoted to the chemistry, biology, and potential medical applications, Ever since the initial reports of these antibiotics in 1980s. Synthetic chemists and molecular designers have been engaged in attempts to synthesize these molecules and to model their unique architecture. Considerable efforts have been directed at understanding and mimicking the various processes involved in the targeting, activation, and DNA cleavage associated with these natural products. This thesis pursuits to synthesize some new analogues of enediyne antibiotics in order to understand the structure-activity relationship of these compounds and give more information to modulate them.The synthetic methods to enediyne antibiotics and their analogues have been reviewed in the preface, three routes have been studied in the experiment and the experiment was divided into three parts...