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A solid phase chemistry approach utilizing Mitsunobu chemistry, amine functionalization, and parallel purification was used to produce a diverse library of benzothiophene analogs. These analogs were used to advance the SAR of this class of molecules and give new directions for future studies.

Analogs 3–5 of balanol (−)- 1 , a potent protein kinase C (PKC) inhibitor, were synthesized with the perhydroazepine moiety replaced by a smaller ring. Their in vitro inhibitory activities against PKC revealed a significant relationship between ring size and potency.

Discovery of novel insecticidal gene products is essential for pest-control strategies using genetically modified plants. We used an empirical procedure to test filtrates from > 10,000 microbial fermentations to identify proteins active in bioassays on several target insects. Two proteins active in bioassays with green peach aphids, Myzus persicae (Sulzer), were discovered in microbial filtrates. These proteins were active in the bioassay because they modified the dietary sucrose. Consequently, the aphids were either unable to survive on or unwilling to feed on the sucrose-depleted diets. One of these proteins catalyzes the synthesis of tri- and tetra-saccharides from sucrose, indicating that this protein is in the hexosyl-transferase class of enzymes. The other microbial filtrate has invertase like activity. These two types of proteins are not viable candidates for insect control strategies because the modification of sucrose in the phloem of plants would have deleterious effects on the plant.