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AssigneeChina Medical University
InventorsSheng-Chu KUO, Che-Ming Teng, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Chih-Shiang Chang, Chung-Ming Sun, Tian-Shung Wu, Shiow-Lin Pan, Tzong-Der Way, Jang-Chang Lee, Jing-Gung Chung, Jai-Sing Yang, Chien-Ting Chen, Ching-Che Huang, Shih-Ming Huang
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2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.
A compound of 2-phenyl-4-quinolone having the following formula IIa:
The compound according to claim 1, wherein R4 is (CH2)qNR8R9, and R2, R3 and R5 are H, wherein q, R8 and R9 are defined as in claim 30.
The compound according to claim 1, wherein R5′ is (CH2)qNR8R9, and R2′, R3′, R4′ and R6′ are H, wherein q, R8 and R9 are defined as in claim 30.
A method for killing cancer cells, which comprises administering to a subject a therapeutically effective amount of a compound R2′, R3′, R4′, R5′ and R6′ (CH2)qNR8R9, wherein X is F, CL or Br, q is an integer of 1-4, R8 and R9 independently are H or (CH2)nCH3, wherein n I s integer of 0-4 of 2-phenyl 4-quinolone as in claim 30 or a pharmaceutically acceptable salt thereof, wherein the cancer cells comprise leukemia cancer.
Dependencies are inferred from the claim text.