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The total synthesis of C25-benzyloxy epothilone C is described. A sequential Suzuki–Aldol–Yamaguchi macrolactonization strategy was utilized employing a novel derivatized C8–C12 fragment. The C25-benzyloxy analog exhibited significantly reduced biological activity in microtubule assembly...
The synthesis of three novel 3′- N - tert -butylsulfonyl analogues of docetaxel 10a – c with potent cytotoxicity against several human tumor cell lines is reported.
The synthesis and biological profile of imidazole carboxamides of general structure 6 as potent and selective cholecystokinin 1 receptor (CCK1R) agonists are described.
The structure–activity relationship of the 2-, 5-, and 6-position of 1,4-dihydropyridine-3-carboxylic acid-derived N-type calcium channel blockers is reported.
The optimization of an HTS-derived hit compound into a potent and metabolically stable MCH-R1 antagonist is described.
Peptidomimetic with P 2 α-aminocyclopentane carboxylic acid. μ-Calpain inhibition, K i = 1.94 μM, cathepsin B inhibition, K i = 0.88 μM. Peptidomimetic with P 2 α,α′-diethylglycine. μ-Calpain inhibition, K i = 0.08 μM, cathepsin B inhibition, K i = 2.91 μM.
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