- Synthesis of neocryptolepines and carbocycle-fused quinolines and evaluation of their anticancer and antiplasmodial activities
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This study reported the discovery of novel compounds containing five-membered ring fused quinoline core structures as anticancer and antimalarial agents. Two libraries containing these core structures, neocryptolepines and carbocycle-fused quinolines, were prepared and evaluated. Compound 3h was found to be much more potent than other analogs against cancer cell lines with high selectivity. Meanwhile, carbocycle-fused quinolines 5h and 5s showed moderate anticancer properties but much less cytotoxicity to normal cell than doxorubicin. In addition, compound 3h also showed much lower cytotoxic against human normal kidney cell line compared to doxorubicin standard. However, only compounds 3s and 3p provided acceptable results for antimalarial activities.
- Akkachairin, Bhornrawin,Mungthin, Mathirut,Reamtong, Onrapak,Rodphon, Warabhorn,Ruchirawat, Somsak,Thongsornkleeb, Charnsak,Tummatorn, Jumreang
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- Domino N2-Extrusion-Cyclization of Alkynylarylketone Derivatives for the Synthesis of Indoloquinolines and Carbocycle-Fused Quinolines
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New synthetic approaches for the synthesis of indoloquinolines and carbocycle-fused quinolines have been developed employing alkynylketone substrates. These synthetic transformations involved the application of N2-extrusion of azido complexes as a key step to generate carbodiimidium ion and nitrilium ion in situ, which further cyclized intramolecularly with alkyne via a domino process to provide indoloquinolines and carbocycle-fused quinolines, respectively, in moderate to good yields.
- Akkachairin, Bhornrawin,Tummatorn, Jumreang,Khamsuwan, Narumol,Thongsornkleeb, Charnsak,Ruchirawat, Somsak
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p. 11254 - 11268
(2018/09/06)
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- 4 + 1 Radical Annulations with Isonitriles: A Simple Route to Cyclopenta-Fused Quinolines
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Sunlamp irradiation of 1-substituted 5-iodo-1-pentynes, 5 equiv of phenyl isocyanide, and 1.5 equiv of hexamethylditin in tert-butylbenzene (0.01-0.025 M) at 150°C produces 9-substituted 2,3-dihydro-1H-cyclopenta[b]quinolines in 36-70% yields. A mechanist
- Curran, Dennis P.,Liu, Hui
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p. 2127 - 2132
(2007/10/02)
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