111964-21-7Relevant articles and documents
Ni-catalyzed direct carboxylation of an unactivated C-H bond with CO2
Pei, Chunzhe,Zong, Jiarui,Han, Shanglin,Li, Bin,Wang, Baiquan
, p. 6897 - 6902 (2020)
The transition-metal-catalyzed direct carboxylation of an unactivated C-H bond is rarely reported, and no example of catalysis using abundant and cheap nickel has been reported. In this work, the first Ni-catalyzed direct carboxylation of an unactivated C-H bond under an atmospheric pressure of CO2 is reported. This method affords moderate to high carboxylation yields of various methyl carboxylates under mild conditions. Preliminary mechanistic studies reveal that a Ni(0)-Ni(II)-Ni(I) catalytic cycle may be involved in this reaction.
Novel inhibitors of Staphylococcus aureus RnpA that synergize with mupirocin
Lounsbury, Nicole,Eidem, Tess,Colquhoun, Jennifer,Mateo, George,Abou-Gharbia, Magid,Dunman, Paul M.,Childers, Wayne E.
supporting information, p. 1127 - 1131 (2018/02/21)
We recently discovered RnpA as a promising new drug discovery target for methicillin-resistant S. aureus (MRSA). RnpA is an essential protein that is thought to perform two required cellular processes. As part of the RNA degrasome Rnpa mediates RNA degradation. In combination with rnpB it forms RNase P haloenzymes which are required for tRNA maturation. A high throughput screen identified RNPA2000 as an inhibitor of both RnpA-associated activities that displayed antibacterial activity against clinically relevant strains of S. aureus, including MRSA. Structure-activity studies aimed at improving potency and replacing the potentially metabotoxic furan moiety led to the identification of a number of more potent analogs. Many of these new analogs possessed overt cellular toxicity that precluded their use as antibiotics but two derivatives, including compound 5o, displayed an impressive synergy with mupirocin, an antibiotic used for decolonizing MSRA whose effectiveness has recently been jeopardized by bacterial resistance. Based on our results, compounds like 5o may ultimately find use in resensitizing mupirocin-resistant bacteria to mupirocin.
Design and synthesis of 2-(3-benzo[b]thienyl)-6,7-methylenedioxyquinolin-4- one analogues as potent antitumor agents that inhibit tubulin assembly
Chang, Yu-Hsun,Hsu, Mei-Hua,Wang, Sheng-Hung,Huang, Li-Jiau,Qian, Keduo,Morris-Natschke, Susan L.,Hamel, Ernest,Kuo, Sheng-Chu,Lee, Kuo-Hsiung
experimental part, p. 4883 - 4891 (2010/02/28)
As part of our continuing investigation of azo-flavonoid derivatives as potential anticancer drug candidates, a series of 2-aryl-6,7- methylenedioxyquinolin-4-one analogues was designed and synthesized. The design combined structural features of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4- one (CHM-1), a previously discovered compound with potent in vivo antitumor activity, and 2-arylquinolin-4-ones, identified by CoMFA models. The newly synthesized analogues were evaluated for cytotoxicity against seven human cancer cell lines, and structure -activity relationship (SAR) correlations were established. Analogues 1, 37, and 39 showed potent cytotoxicity against different cancer cell lines. Compound 1 demonstrated selective cytotoxicity against Hep 3B (hepatoma) cells. Compound 37 was cytotoxic against HL-60 (leukemia), HCT-116 (colon cancer), Hep 3B (hepatoma), and SK-MEL-5 (melanoma) cells. Compound 39 exhibited broad cytotoxicity against all seven cancer cell lines, with IC50 values between 0.07 and 0.19 μM. Results from mechanism of action studies revealed that these new quinolone derivatives function as antitubulin agents.