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The interactions of epothilone analogs with the paclitaxel binding site of microtubules were studied. The influence of chemical modifications in the C15 side chain and in C12 on binding affinity and microtubule elongation was characterized. Modifications favorable for binding affinity are (1). a thiomethyl group at C21 of the thiazole side chain, (2). a(More)
Owing to their potent cytotoxicity against tumor cells, including taxol (paclitaxel)-resistant cell lines, the epothilones (for example, epothilone A (1) and epothilone B (2)) [1] continue to be the focus of intense chemical, biological, and clinical research efforts around the world. [2, 3] Following the findings that cyclopropane-, [4](More)
Kappa opioid receptor (KOR) is an important mediator of pain signaling and it is targeted for the treatment of various pains. Pharmacophore based mining of databases led to the identification of 2-aminobenzimidazole derivative as KOR agonists with selectivity over the other opioid receptors DOR and MOR. A short SAR exploration with the objective of(More)
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