Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.

Evasion of apoptosis is critical for the development and growth of tumors. The pro-survival protein myeloid cell leukemia 1 (Mcl-1) is an antiapoptotic member of the Bcl-2 family, associated with tumor aggressiveness, poor survival, and drug resistance. Development of Mcl-1 inhibitors implies blocking of protein-protein interactions, generally requiring a lengthy optimization process of large, complex molecules.

Protective group-free synthesis of 3,4-dihydroxytetrahydrofurans from carbohydrates: formal total synthesis of sphydrofuran.

Carbohydrates are taking a more prominent role in chemistry as an environmentally benign chemical feedstock. However, major efforts are still required to convert unprotected carbohydrates into high-value building blocks. We have investigated the protective group-free Wittig reaction and subsequential acid catalyzed intramolecular cyclization of unprotected carbohydrates to obtain 3,4-dihydroxytetrafurans.