- Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach
-
BPR0L075 (2) is a potential anticancer drug candidate designed from Combretastatin A-4 (1) based on the bioisosterismprinciple.Metabolites of 2, proposed from in vitrohumanmicrosome studies,were synthesized, leading to the identification of metabolite-der
- Wu, Yu-Shan,Coumar, Mohane Selvaraj,Chang, Jang-Yang,Sun, Hsu-Yi,Kuo, Fu-Ming,Kuo, Ching-Chuan,Chen, Ying-Jun,Chang, Chi-Yen,Hsiao, Chia-Ling,Liou, Jing-Ping,Chen, Ching-Ping,Yao, Hsien-Tsung,Chiang, Yi-Kun,Tan, Uan-Kang,Chen, Chiung-Tong,Chu, Chang-Ying,Wu, Su-Ying,Yeh, Teng-Kuang,Lin, Chin-Yu,Hsieh, Hsing-Pang
-
supporting information; experimental part
p. 4941 - 4945
(2010/03/02)
-
- Synthesis and antiproliferative in-vitro activity of natural flavans and related compounds
-
The total synthesis of natural flavan racemates (±) 1, (±) 2 and natural flavones 3, 4 had thus been achieved. A straightforward synthetic procedure of flavans via the Pd-C catalyzed hydrogenation/hydrogenolysis of corresponding flavones was developed. Furthermore, the antiproliferative activities of racemic flavans (±) 1, (±) 2, flavones 3, 4, and five synthetic intermediates toward human SGC-7901, BEL-7402, HeLa, and HL-60 cell lines in vitro were evaluated by MTT assay, and the racemic flavans (±) 1 were found to have significant antiproliferative activity against all four cell lines.
- Zhang, Liang,Zhang, Wei-Ge,Ma, En-Long,Wu, Lan,Bao, Kai,Wang, Xiao-Long,Wang, Yu-Ling,Song, Hong-Rui
-
p. 650 - 655
(2008/12/21)
-
- Synthesis and PAF antagonist activity of some 2,5-diaryltetrahydrofurans incorporating PAF-like functional groups
-
This paper describes the synthesis and structure-activity relationships of a series of 2,5-diaryltetrahydrofurans, as specific and potent antagonists at the rabbit washed platelet activating factor (PAF) receptor. The methoxyl groups in the known PAF antagonist L-652,731 were replaced with functional groups present in PAF and in the 'PAF-like' antagonists. Activity was generally retained or enhanced when one aryl ring in L-652,731 was elaborated; however incorporation of these functional groups into both of the aryl rings greatly reduced or abolished activity. These results are discussed in relation to a putative model for the PAF receptor.
- Smith,Blackwell,Demaine,Garland,Hodson,Hyde,Parke,Rose,Sawyer,Tilling
-
p. 347 - 358
(2007/10/03)
-