Design, synthesis and evaluation of novel indole derivatives as AKT inhibitors.

Herein, we describe the discovery and synthesis of a new series of 1,2,4,7-tetra-substituted indole derivatives as novel AKT inhibitors by optimization of a weak hit methyl 4-(2-aminoethoxy)-1H-indole-2-carboxylate (1). Both representative compounds 6a and 6o exhibited the most potent inhibitory activities against AKT1, with inhibition rates of 72.5% and 78.

Methyl 4-benz-yloxy-7-meth-oxy-1-methyl-1H-indole-2-carboxyl-ate.

There are two independent mol-ecules in the asymmetric unit of the title compound, C(19)H(19)NO(4). The indole unit in each mol-ecule is essentially planar, with mean deviations of 0.017 (1) and 0.

Synthesis and anticancer activity of novel 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles.

A new series of 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles were synthesized and evaluated for their anticancer activities. Structures of the compounds were confirmed by spectroscopic methods. Structural modifications were done to improve the antiproliferative activity of compound 1.