Design and Synthesis of Mycophenolic Acid Analogues for Osteosarcoma Cancer Treatment.

Mycophenolic acid (MPA), a natural compound, was modified to new MPA analogues via the classical method of silylation and esterification. Their cytotoxicity was evaluated in vitro on four osteosarcoma cancer cell lines (MNNG/HOS, U2OS, 143B, and SaOS-2) and human normal cells (hFOB 1.19).

Visible-light-induced photocatalytic four-component fluoroalkylation-dithiocarbamylation difunctionalization of styrenes.

Herein we demonstrate that a visible-light-induced photocatalytic four-component fluoroalkylation-dithiocarbamylation is a unified method for the fluoroalkylation of diverse activated fluoroalkyl halides, including monofluoroalkyl bromides, difluoroalkyl bromides, trifluoromethyl iodide, and perfluoroalkyl iodides. The synthetic value of this method has been demonstrated by the transformations of various substrates containing drug/natural product skeletons, gram scale reactions, and further derivatizations of the fluorodithiocarbamate products. This work features an atom economical protocol that is simple to operate, does not require any additives or strong bases, and can be carried out under mild conditions.

Genipin Analogue (G300) Inhibits Adipogenic Differentiation of Human Bone Marrow-Derived Mesenchymal Stem Cells through the Suppression of Adipogenic Promoting Factors.

While obesity is a well-known health threatening condition worldwide, effective pharmacological interventions for obesity suppression have been limited due to adverse effects. Therefore, it is important to explore alternative medical treatments for combating obesity. Inhibition of the adipogenesis process and lipid accumulation are critical targets for controlling and treating obesity.

Divergent Synthesis of 3-Pyrrolidin-2-yl-1-indoles, Symmetric and Unsymmetric Bis(Indolyl)Methanes (BIMs) through Photocatalyzed Decarboxylative Coupling/Friedel-Crafts Alkylation Reaction.

This paper reports the acid-controlled divergent synthesis of 3-pyrrolidin-2-yl-1-indoles and symmetric and unsymmetrical bis(indolyl)methanes (BIMs) through photocatalyzed decarboxylative coupling and Friedel-Crafts alkylation reactions, respectively. The protocol involves C-H functionalization, switching formation of two products, room-temperature conditions, low photocatalyst loadings, without strong oxidant, and moderate to excellent yields. This method has been applied for the synthesis of natural product vibrindole A and 1,1-bis(1-indol-3-yl)-2-phenylethane.

New 1,2,3-Triazole-genipin Analogues and Their Anti-Alzheimer's Activity.

A novel series of 1,2,3-triazole-genipin analogues were designed, synthesized, and evaluated for neuroprotective activity, acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE) inhibitory activity. The genipin analogues bearing bromoethyl- and diphenylhydroxy-triazole showed neuroprotective properties against HO toxicity along with potent inhibitory activity on BuChE with IC values of 31.77 and 54.

Synthesis of propargylamine mycophenolate analogues and their selective cytotoxic activity towards neuroblastoma SH-SY5Y cell line.

Twenty six propargylamine mycophenolate analogues were designed and synthesized from mycophenolic acid 1 employing a key step A-coupling reaction. Their cytotoxic activity was examined against six cancer cell lines. Compounds 6a, 6j, 6t, 6u, and 6z exhibited selective cytotoxicity towards neuroblastoma (SH-SY5Y) cancer cells and were less toxic to normal cells in comparison to the lead compound, MPA 1 and a standard drug, ellipticine.

Hypervalent-Iodine(III)-Mediated Tandem Oxidative Dearomatization/Aziridination of Phenolic Amines: Synthesis of Functionalized Unactivated Aziridines.

A new hypervalent-iodine(III)-mediated tandem reaction involving oxidative dearomatization and in situ aziridination of phenolic amines is described, providing a mild and effective method for the assembly of structurally interesting and synthetically useful aziridines. Importantly, the densely functionalized aziridines resulting from this unprecedented tandem reaction offer a platform for expeditious access to architecturally diverse aza-heterocycles through transformations initiated by selective ring-opening of aziridines.

Synthetic analogues of durantoside I from Citharexylum spinosum L. and their cytotoxic activity.

New iridoid glycoside derivatives from durantoside I, the latter from the dried flowers and leaves of Citharexylum spinosum, were synthesized by variously modifying a sugar moiety by silylation or acetylation and/or removal of cinnamate group at C-7 position and subsequent screening for comparative cytotoxicity against several cancer cell lines. Addition of alkylsilane to durantoside I and removal of cinnamate group were most effective in improving cytotoxicity.