Yaping Lv

Synthesis and antitumor activity of feruloyl and caffeoyl derivatives

We developed two efficient protocols for the synthesis of feruloyl and caffeoyl derivatives from commercial vanillin and veratraldehyde. Pharmacological activities were assessed against a panel of human cancer cell lines in vitro. Most synthesized compounds demonstrated attractive cytotoxicity. Several new compounds demonstrated significant antiproliferative and cytotoxic activities against HeLa and Bewo tumor cell lines. In particular, 5-nitro caffeic adamantyl ester showed broad spectrum of tumor inhibition in 10 cell lines, and reduced tumor weight by 36.7% in vivo when administered at a dose of 40 mg kg(-1).

Metal-Oxidant-Free Cobalt-Catalyzed C(sp2)–H Carbonylation of ortho-Arylanilines: An Approach toward Free (NH)-Phenanthridinones

A traceless directing group assisted Co-catalyzed C(sp2)-H carbonylation of ortho-arylanilines for the synthesis of free ( NH)-phenanthridinones in metal-based-oxidant-free fashion was accomplished. This protocol employs diisopropyl azodicarboxylate as the CO source and oxygen as the sole oxidant, and provides good yields with various functional tolerance. The methodology has been applied for the total synthesis of PARP inhibitor PJ-34. Furthermore, the kinetic isotopic effect experiments reveal the C-H bond cleavage probably occurred in the rate-determining step.

Macrocalyxin A inhibits proliferation and induces apoptosis of t (8;21) leukemia cells through mitochondrial signaling pathways and regulates AML‑ETO mRNA expression

Progress in the last decade has improved the treatment of acute myeloid leukemia (AML); however, the treatment of AML is also demanding and better treatments are required. The present study aimed to examine the antiproliferative and proapoptotic effects of macrocalyxin A (MA), a novel deterpenid compound, on AML cells. It was identified that MA significantly inhibits kasumi‑1 cell proliferation in a time‑ and dose‑dependent manner. Furthermore, low concentrations of MA were able to induce kasumi‑1 cell differentiation; however, high concentrations of MA induced kasumi‑1 cell apoptosis. MA was also able to increase the expression of mitochondrial membrane protein in a dose‑dependent manner while the ∆Ψm was reduced. Additionally, Bad expression in kasumi‑1 cells was increased when treated with MA, indicating that the intrinsic apoptotic pathway may be important in MA‑induced kasumi‑1 cell apoptosis, where the mitochondrial permeability transition pore is opened and the ΔΨm is reduced. In addition, it was demonstrated that AML‑ETO mRNA may also be important in MA‑induced apoptosis.

Development of Ferrocene-Based Diamine-Phosphine-Sulfonamide Ligands for Iridium-Catalyzed Asymmetric Hydrogenation of Ketones

A series of air-stable, easily accessible tridentate ferrocene-based diamine-phosphine sulfonamide (f-diaphos) ligands were successfully developed for iridium-catalyzed asymmetric hydrogenation of ketones. The f-diaphos ligands exhibited excellent enantioselectivity and superb reactivity in Ir-catalyzed asymmetric hydrogenation of ketones (for arylalkyl ketones, ( S)-selectivity, up to 99.4% ee, and 100 000 TON; for diaryl ketones, ( R)-selectivity, up to 98.2% ee, and 10 000 TON). This protocol could be easily conducted on gram scale, thereby providing a chance to various drugs.