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
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2016年 / 13卷 / 06期
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
相关论文
共 50 条
  • [1] SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NEW COUMARIN DERIVATIVES AS ANTIMICROBIAL AGENTS
    Youssif, Bahaa Gamal Mohamed
    [J]. BULLETIN OF PHARMACEUTICAL SCIENCES, 2013, 36 : 104 - 116
  • [2] SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NEW RUTIN SEMISYNTHETIC DERIVATIVES AS ANTIBACTERIAL AGENTS
    Lupascu, Dan
    Tuchilus, Cristina
    Lupusoru, Catalina Elena
    Ghiciuc, Cristina
    Sutu, Maria
    Neagu, Alexandra
    Profire, Lenuta
    [J]. FARMACIA, 2012, 60 (04) : 556 - 564
  • [3] Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents
    Altintop, Mehlika Dilek
    Ozdemir, Ahmet
    Turan-Zitouni, Gulhan
    Ilgin, Sinem
    Atli, Ozlem
    Iscan, Gokalp
    Kaplancikli, Zafer Asim
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2012, 58 : 299 - 307
  • [4] Design, Synthesis and Biological Evaluation of Some New Coumarin Derivatives as Potential Antimicrobial Agents
    Singh, Lav Kumar
    Priyanka
    Singh, Vineeta
    Katiyar, Diksha
    [J]. MEDICINAL CHEMISTRY, 2015, 11 (02) : 128 - 134
  • [5] Synthesis and biological evaluation of some new furoxan derivatives as anti-inflammatory agents
    Amir, Mohd
    Verma, Jeevan S.
    Tariq, Sana
    Somakala, K.
    Haq, S. Ehtaishamul
    [J]. INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 2018, 57 (07): : 955 - 959
  • [6] Synthesis and biological evaluation of some new pyrazoline derivatives as anti-inflammatory agents
    Amir, Mohd
    Ali, Sazid
    Somakala, K.
    [J]. INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 2016, 55 (04): : 478 - 485
  • [7] SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NEW HETEROCYCLIC DERIVATIVES OF CHALCONE AS ANTIHYPERGLYCEMIC AGENTS
    Jain, A.
    Jain, D. K.
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, 2019, 10 (12): : 5700 - 5706
  • [8] Synthesis and biological evaluation of some new chalcones and their derivatives
    Solankee, A
    Kapadia, K
    Thakor, I
    Patel, J
    Lad, S
    [J]. ASIAN JOURNAL OF CHEMISTRY, 2004, 16 (02) : 921 - 927
  • [9] SYNTHESIS, BIOLOGICAL EVALUATION OF SOME NEW THIOPHENE DERIVATIVES
    Abu-Melha, Sraa
    [J]. HETEROCYCLES, 2016, 92 (07) : 1261 - 1271
  • [10] Synthesis and biological evaluation of some new coumarin derivatives
    Al-Haiza, MA
    Mostafa, MS
    El-Kady, MY
    [J]. MOLECULES, 2003, 8 (02) : 275 - 286
12345