Consequently, numerous efforts have been devoted to the formation of three-membered carbocyclic rings during the last few decades. For instance, the ring-enlargement reactions of cyclopropanes with nucleophiles, such as amines, alcohols, and carboxylic acids, are efficient pathways to various heterocycles. Meanwhile, cyclopropanes can also be applied as versatile units for the construction of other frameworks due to their unique combination of reactivity and structural properties. also exhibited biological activities for example, the OPH carboxylic acid can affect the function of disintegrin and metalloproteinase domain-containing proteins. Other compounds reported by Berman et al. For instance, ledipasvir, a drug developed by Gilead Sciences, is an effective inhibitor of the hepatitis C virus.
Recently, many spirocyclopropanes possessing a pyrrolidin-2-one moiety have been developed into useful drug candidates. The natural products CC-1065, duocarmycin A and AS were identified as strong anticancer drug candidates as well. Ptaquiloside, a toxic derivative from bracken, is recently reported to depress tumor-infiltration in HPV-16 transgenic mice. For example, the illudins, sesquiterpene secondary metabolites of basidiomycetes, have demonstrated activity against cancer acylfulvene and irofulven, which are derived from illudin via a semisynthetic approach, also show anti-tumor bioactivity. Among various spirocycles, spirocyclopropanes have shown high potential pharmaceutical activities ( Figure 1). Due to their important physiological functions, the synthesis of spirocycles has become an attractive target in organic chemistry, especially in recent years. Spirocycles are significant structures found in various natural products and many potent synthetic drug candidates.
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