Henry, Kenneth J. Jr. published the artcileDiscovery of a Series of Cyclohexylethylamine-Containing Protein Farnesyltransferase Inhibitors Exhibiting Potent Cellular Activity, Synthetic Route of 165534-79-2, the publication is Journal of Medicinal Chemistry (1999), 42(23), 4844-4852, database is CAplus and MEDLINE.
Synthesis of a library of secondary benzylic amines based on the Sebti-Hamilton type peptidomimetic farnesyltransferase (FTase) inhibitor FTI-276 led to the identification of [(I); R = H] as a potent enzyme inhibitor (IC50 of 8 nM) which lacked the problematic thiol residue which had been a common theme in many of the more important FTase inhibitors reported to date. It has previously been disclosed that addition of o-tolyl substitution to FTase inhibitors of the general description (II) had a salutary effect on both FTase inhibition and inhibition of Ras prenylation in whole cells. Combination of these two observations led us to synthesize [I; R = Me(III)], a potent FTase inhibitor which displayed an IC50 of 0.16 nM for in vitro inhibition of FTase and an EC50 of 190 nM for inhibition of whole cell Ras prenylation. Modification of III by classical medicinal chem. led to the discovery of a series of potent FTase inhibitors, culminating in the identification of (IV) which exhibited an IC50 of 0.20 nM and an EC50 of 4.4 nM. In vivo tests in a nude mouse xenograft model of human pancreatic cancer (MiaPaCa cells) showed that oral dosing of IV gave rise to impressive attenuation of the growth of this aggressive tumor cell line.
Journal of Medicinal Chemistry published new progress about 165534-79-2. 165534-79-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Benzene,Ester, name is Dimethyl 2-iodoterephthalate, and the molecular formula is C10H9IO4, Synthetic Route of 165534-79-2.
Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com