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ABSTRACT: In search of more potent anticancer agents, 15 nitric oxide (NO)-donating thalidomide analogues, 6a, 6b, 8a-8e, and 13a-13h, were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against three human tumor cell lines (HepG2, A549, and PC-3). The results indicated that 13a-13d exhibited notable anticancer activities comparable to or stronger than that of 5-fluorouracil (5-FU). Structure-activity relationships were also discussed, based on the experimental data obtained. Generally, the cytotoxic activity of target compounds is closely related to the type of NO donors, and the length of the spacers connecting to NO donors also appears important for the bioactivities.
Chemistry & Biodiversity 05/2009; 6(4):466-74. · 1.80 Impact Factor
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ABSTRACT: In search of novel anticancer agents, two series of dimethyl [1,1'-biphenyl]-2,2'-dicarboxylate derivatives, 8a-8k and 9a-9k, containing both methylenedioxy and 1,3,4-thiadiazole moieties were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against five human tumor cell lines, i.e., HepG2, KB, A549, K562, and MCF-7. The results indicated that 8h, 8j, 8k, 9d, 9g, 9h, 9j, and 9k showed notable anticancer activities comparable to or stronger than that of 5-fluorouracil, a canonical anticancer drug. Structure-activity relationships were also discussed based on the experimental data obtained.
Chemistry & Biodiversity 10/2008; 5(9):1743-52. · 1.80 Impact Factor
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ABSTRACT: In search of novel anticancer agents, a series of thalidomide analogs (6a–j) were designed and synthesized. Cytotoxicity of these compounds against human hepatoma cells (HepG2) was evaluated by MTT method. Compounds 6d, 6h and 6i showed significant cytotoxic activities comparable to or stronger than control 5-fluorouracil.
Chinese Chemical Letters 19(8):928-930. · 0.98 Impact Factor
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ABSTRACT: Novel phthalimide derivatives (4a, 4b and 6a–6e) were designed as hybrids of thalidomide and NO-ASA, and their chemical synthesis and in vitro biological activities were presented. The preliminary results showed that compared to thalidomide 4a and 4b exhibited enhanced activities against ECV304 and HepG2 cells, whereas 6c was more potent against HepG2 cells.
Chinese Chemical Letters 19(1):26-28. · 0.98 Impact Factor
