Synthesis and biological evaluation of novel hybrid compounds between chalcone and piperazine as potential antitumor agents

Abstract

A series of novel hybrid compounds between chalcone and piperazine have been synthesized, and their in vitro antitumor activity was evaluated against a panel of human tumor cell lines by MTT assay.

Design, synthesis and anticancer activity of novel hybrid compounds between benzofuran and N-aryl piperazine

“…11 Moreover, in previous research, we have designed hybrid compounds between chalcone and N-aryl piperazine with excellent cytotoxic activities. 12 On the basis of these results, we were interested in designing and synthesizing a number of novel hybrid compounds bearing 2-phenzoyl benzofuran and N-aryl piperazine moieties (Scheme 1).…”

“…The corresponding benzofuran-N-aryl piperazine derivative (4) 14 was prepared from compound (3) by substitution with piperazine in the presence of Cs 2 CO 3 at 110 o C in DMF in 82% yield. Based on our previous synthesis, the desired compounds (5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20) were prepared with excellent yields by reaction of intermediate (4) with acyl chloride, carboxylic acid or sulfonyl chloride. Comparative data for novel hybrid compounds with respective to structures and yield are provided in Table 1.…”

New indolizine–chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation

“…[19][20][21] Increasing interest is currently given especially to hybrids of chalcones with different heterocycles. 19 However, very few chalcones were described in the literature as farnesyltransferase inhibitors and exhibited moderate efficacy.…”

Synthesis and Anti-tumor Activities of Novel 4'-(N-Substitued-1-piperazinyl) chalcone Derivatives

“…活性结果表明, 当哌嗪环上 N-H 被苯乙酮取代时, 其细胞毒活性明显增强 [16] , 如图 1 所 示. 图式 1 查尔酮-哌嗪衍生物的合成路线 Scheme 1 Synthetic route of chalcone-piperazine derivatives 1 结果与讨论 …”