1,2-Diaryloxyethene has recently been proposed as a linker in singlet oxygen-mediated drug release. Even though 1,2-diaryloxyethenes look very simple, their synthesis was not an easy task. Previous methods are limited to symmetric molecules, lengthy step and low yield. We report on a facile synthetic method not only for 1,2-diaryloxyethenes but also their sulfur and nitrogen analogs in yields ranging from 40 to 90% with more than 90% purity at the vinylation reaction.

Polyoxins and nikkomycins are a class of naturally occurring peptidyl nucleoside antibiotics that show promise as potential antifungal agents due to their potent ability to inhibit chitin synthase, an enzyme responsible for fungal cell wall biosynthesis. Whole cell assays and in vivo studies have shown that these natural products have poor cellular uptake and are metabolically unstable, and there has been a concerted effort to improve their pharmokinetic properties by synthesizing analogs. These have either been designed as natural substrate analogs, transition state mimetics or mechanistic inhibitors. Recent synthetic efforts and the results of their biological studies are briefly described in this review, and the current trends in the design and construction of polyoxin and nikkomycin analogs are discussed.

No abstract

As a continuation of our efforts to develop the benzimidazole-PBD conjugates as potential anticancer agents, a series of heteroaryl substituted benzimidazole linked PBD conjugates has been synthesized and evaluated for their anticancer potential in 60 human cancer cell lines. Most of the compounds exhibited promising anticancer activity and interestingly, compounds 4c and 4d displayed significant activity in most of the cell lines tested. Whereas, compound 4e showed selectivity in renal cancer cells with GI50 values of <10 and 70 nM against RXF 393 and UO-31 cell lines, respectively. Further, these compounds also showed significant DNA-binding affinity by thermal denaturation study using duplex form of calf thymus (CT) DNA.