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An efficient one-pot reaction for the synthesis of oxoaporphine alkaloids has been developed. Twenty-three compounds of oxoaporphine alkaloids were prepared and assessed for their antitumor activities. Most compounds inhibited the growth of T-24 tumor cells in vitro. Particularly, 4B displayed the most potent activity with an IC 50 value of 0.5 μM, which was 19-fold more potent than the parent compound 4. The substitution at C3-position of oxoaporphine core by -NO 2 significantly enhanced the anticancer activity. Mechanism studies indicated that 4 and 4B induced cell cycle arrest at G2/M phase; in contrast, 4V induced cell cycle arrest at the S phase. Increase of mitochondrial ROS/Ca 2+ and decrease of MMP, accompanied by activation of caspase-3/9, were observed in T-24 cells after exposure to compounds 4, 4B and 4V, suggesting that the mitochondrial pathway was involved in the induced apoptosis. Moreover, compound 4B effectively inhibited tumor growth in a mouse xenograft model bearing T-24., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2022 Elsevier Masson SAS. All rights reserved.)

A metal-free and efficient visible-light-induced spirocyclization of indolyl-ynones with diselenides at room temperature under air atmosphere to prepare 3-selenospiroindolenines in moderate to good yields has been developed. The resulting products were tested for in vitro anticancer activity by MTT assay, and compounds 3 c and 3 e showed potent cancer cell-growth inhibition activities., (© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

N‐(α‐alkoxyalkyl)benzotriazoles are of great importance for biochemical and antitumor activity. A feasible protocol has been developed for the synthesis of N‐(α‐alkoxyalkyl)benzotriazoles using azoles, aldehydes and alcohols as substrates under electrochemical conditions. The reaction is carried out under acid catalyst‐ and oxidant‐free conditions, so that a variety of synthetically useful nitrogen heterocyclic derivatives can be obtained. More meaningfully, a gram‐scale synthetic approach was employed to demonstrate the scale‐up applicability of this transformation. [ABSTRACT FROM AUTHOR]

Synthesis of organotellurium compounds is crucial in pharmaceutical sciences. Herein, a novel and efficient electrochemically catalyzed multicomponent reaction of propargylamide or propargylamine with CO2 and ditellurium has been developed, and a variety of tellurium-containing 2-oxazolidinones were synthesized for the first time to the best of our knowledge with satisfactory yields under mild conditions. In addition, the resulting tellurium-containing 2-oxazolidinones were tested for in vitro anticancer activity by using the MTT assay against various types of human cancer cells. Compound 5e showed better antitumor activity than did the other oxazolidinone and selenium-containing oxazolidinone compounds. These findings have provided new synthetic strategies for organotellurium compounds and have shown a new perspective for the study of the biological activity of chalcogen-containing organic compounds. [ABSTRACT FROM AUTHOR]

A metal‐free and efficient visible‐light‐induced spirocyclization of indolyl‐ynones with diselenides at room temperature under air atmosphere to prepare 3‐selenospiroindolenines in moderate to good yields has been developed. The resulting products were tested for in vitro anticancer activity by MTT assay, and compounds 3 c and 3 e showed potent cancer cell‐growth inhibition activities. [ABSTRACT FROM AUTHOR]

Breast cancer is a major cause of cancer-related death in women. Antitumor T cell responses play critical therapeutic roles, including direct cytotoxicity mediated by CD8 + T cells and immunomodulatory roles mediated by CD4 + T cells. The IL-9-expressing Th9 cells are recently found to present antitumor immunity in melanoma and lung adenocarcinoma. In this study, we found that IL-9 expression in the serum and in circulating CD4 + T cells were significantly upregulated in breast cancer patients compared to healthy controls. The IL-9-expressing Th9 cells were enriched in the CCR4 − CCR6 − CXCR3 − subset. Upon TCR stimulation, this subset also presented potent IL-10 and IL-21 expression in addition to IL-9 expression. CCR4 − CCR6 − CXCR3 − CD4 + T cells also assisted in the killing of autologous tumor cells by CD8 + T cells, but did not initiate cytotoxicity by themselves. This enhancement in CD8 + T cell-mediated cytotoxicity was dependent on IL-9 as well as on IL-21. Interestingly, the tumor-infiltrating Th9 cells presented comparable IL-9, reduced IL-10, and elevated IL-21 expression compared with their counterparts in the peripheral blood. Together, these results demonstrated that IL-9-expressing Th9 cells were upregulated in breast cancer patients and potentially possessed antitumor roles by enhancing CD8 + T cell-mediated cytotoxicity. [ABSTRACT FROM AUTHOR]