Zhao, Min published the artcileSynthesis and evaluation of new compounds bearing 3-(4-aminopiperidin-1-yl)methyl magnolol scaffold as anticancer agents for the treatment of non-small cell lung cancer via targeting autophagy, COA of Formula: C10H20N2O2, the main research area is magnolol aminopiperidinylmethyl preparation anticancer non small cell lung cancer; Autophagy; Magnolia officinalis; Magonolol; Non-small cell lung cancer.
Magnolol and honokiol are the two major active ingredients with similar structure and anticancer activity from traditional Chinese medicine Magnolia officinalis, and honokiol is now in a phase I clin. trial (CTR20170822) for advanced non-small cell lung cancer (NSCLC). In search of potent lead compounds with better activity, our previous study has demonstrated that magnolol derivative 3-(4-aminopiperidin-1-yl)methyl magnolol has better activity than honokiol. Here, based on the core of 3-(4-aminopiperidin-1-yl)methyl magnolol, we synthesized fifty-one magnolol derivatives Among them, compound I exhibited the most potent antiproliferative activities on H460, HCC827, H1975 cell lines with the IC50 values of 0.63-0.93μM, which were approx. 10- and 100-fold more potent than those of C2 and magnolol, resp. Besides, oral administration of I and C2 on an H460 xenograft model also demonstrated that I has better activity than C2. Mechanism study revealed that I induced G0/G1 phase cell cycle arrest, apoptosis and autophagy in cancer cells. Moreover, blocking autophagy by the autophagic inhibitor enhanced the anticancer activity of I in vitro and in vivo, suggesting autophagy played a cytoprotective role on I-induced cancer cell death. Taken together, our study implied that compound I combined with autophagic inhibitor could be another choice for NSCLC treatment in further investigation.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, COA of Formula: C10H20N2O2.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem