Abstract: This present invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.

Abstract: The stereochemical centers of a polyketide can be changed by replacement of ketosynthase domains in the polyketide synthase (PKS) enzyme that produces the polyketide. The specificity of the AT domains of a PKS is determined by a hypervariable region that can be replaced or altered to change the specificity of the AT domain from a naturally occurring extender unit to another naturally or non-naturally occurring extender unit. Non-naturally occurring extender units, including methylmalonyl N-acetyl cysteamine thioester can be incorporated into polyketides in recombinant host cells or in cell-free systems to make polyketides.

Abstract: The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; R4 is hydrogen, halogen, C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 haloalkyl, aryl, —C(═O)R6, —C(═O)OR6, —NR6R7 where R6 and R7 are each independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; W is O, NR8 where R8 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; X is O, CH2 or a carbon-carbon double bond; Y is absent or a C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.