Xu, Guoyan G. published the artcileExploration on natural product anibamine side chain modification toward development of novel CCR5 antagonists and potential anti-prostate cancer agents, Application In Synthesis of 20029-52-1, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(17), 3721-3725, database is CAplus and MEDLINE.
Prostate cancer is one of the leading causes of death among males in the world. Prostate cancer cells have been shown to express upregulated chemokine receptor CCR5, a G protein-coupled receptor (GPCR) that relates to the inflammation process. Anibamine, a natural product containing a pyridine ring and two aliphatic side chains, was shown to carry a binding affinity of 1 μM at CCR5 as an antagonist with potential anticancer activity. However, it is not drug-like according to the Lipinski’s rule of five mainly due to its two long aliphatic side chains. In the effort to improve its drug-like property, a series of anibamine derivatives were designed and synthesized by placement of aromatic side chains through an amide linkage to the pyridine ring. The newly synthesized compounds were tested for their CCR5 affinity and antagonism, and potential antiproliferation activity against prostate cancer cell lines. Basal cytotoxicity was finally studied for compounds showing potent antiproliferation activity. It was found that compounds with hydrophobic substitutions on the aromatic systems seemed to carry more promising CCR5 binding and prostate cancer cell proliferation inhibition activities.
Bioorganic & Medicinal Chemistry Letters published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C7H11N, Application In Synthesis of 20029-52-1.
Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider