Synthesis and Biological Evaluation of Some New Indolizine Derivatives as Antitumoral Agents

被引:3
|
作者
Lucescu, Liliana [1 ]
Bicu, Elena [1 ]
Belei, Dalila [1 ]
Dubois, Joelle [2 ]
Ghinet, Alina [1 ,3 ,4 ]
机构
[1] Alexandru Ioan Cuza Univ, Fac Chem, Dept Organ Chem, B Dul Carol 1,11,Corp A, Iasi 700506, Romania
[2] CNRS, Ctr Rech Gif, Inst Chim Subst Nat, UPR2301, Ave Terrasse, F-91198 Gif Sur Yvette, France
[3] Univ Lille 2, INSERM, LIRIC, U995,CHRU Lille,Fac Med Pole Rech, Pl Verdun, F-59045 Lille, France
[4] HEI, Lab Pharmacochim, Ecole Hautes Etud Ingn HEI, 13 Rue Toul, F-59046 Lille, France
关键词
Indolizine; farnesyltransferase; anticancer agent; HUMAN FARNESYLTRANSFERASE; POTENT INHIBITORS; CELL LINE; DISCOVERY; 15-LIPOXYGENASE; CYTOTOXICITY; HETEROCYCLES; ASSAY;
D O I
10.2174/1570180812666151022221628
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new series of indolizine derivatives were synthesized and screened for the antiproliferative potential against NCI 60 tumor cell line panel. The results of the study revealed a selective and good antitumor growth inhibitory activity against SNB-75 CNS cancer cell line for 1-cyanoindolizine derivative 10b. Moreover, a supplementary in vitro biological evaluation showed that compound 9d exhibited a significant farnesyltransferase inhibition activity (IC50 = 1.07 +/- 0.34 mu M) and could represent a lead for the development of new antitumoral chemical entities.
引用
收藏
页码:479 / 488
页数:10
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