Synthesis and Cytotoxicity Studies of Novel 2-Hydrazonylpyrido[2,3-b]pyrazin-3(4H)-ones

被引:6
|
作者
Zhang, Guogang [1 ]
Liu, Yajing [1 ]
Wang, Shuobing [1 ]
Zhou, Chuan [1 ]
Huang, Qingchang [1 ]
Gong, Ping [1 ]
机构
[1] Shenyang Pharmaceut Univ, Key Lab Original New Drugs Design & Discovery, Minist Educ, Sch Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China
关键词
Anticancer activity; Apoptosis; 2-Hydrazonylpyrido[2; 3-b]pyrazin-3(4H)-ones; APOPTOSIS; CALPAIN;
D O I
10.1002/ardp.201100103
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In an attempt to develop potent antitumor agents, a series of novel 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that five of the target compounds showed cytotoxicity against A549 cell line below a concentration of 1 mu M. Compound 15g was the most potent one with IC50 values of 0.19, 2.11 and 2.15 mu M against A549, MDA-MB-231 and HT29 cell lines, respectively.
引用
收藏
页码:49 / 56
页数:8
相关论文
共 50 条
  • [2] Synthesis and in vitro cytotoxic evaluation of 2-hydrazinylpyrido[2,3-b]pyrazin-3(4H)-one derivatives
    Zhang, Guo Gang
    Liu, Ya Jing
    Ma, Xiao Guang
    Dong, Hao
    Li, Ju
    Gong, Ping
    CHINESE CHEMICAL LETTERS, 2011, 22 (10) : 1223 - 1225
  • [3] A series of pyrido[2,3-b]pyrazin-3(4H)-one derivatives as aldose reductase inhibitors with antioxidant activity
    Han, Zhongfei
    Hao, Xin
    Ma, Bing
    Zhu, Changjin
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2016, 121 : 308 - 317
  • [4] Synthesis and nmr structural assignment of 3-benzoylpyrrolo[2,3-b]quinoxalin-2(4H)-ones
    Ostrowska, K
    Zylewski, M
    Walocha, K
    HETEROCYCLES, 2002, 57 (08) : 1413 - 1421
  • [5] Rearrangement of 2-(2-aryl-2-oxoethyl)-1,2-dihydropyrido-[2,3-b]pyrazin- 3(4H)-ones [5]
    V. N. Karazin Kharkiv National University, Kharkiv 61077, Ukraine
    Chem. Heterocycl. Compd., 2007, 10 (1351-1352): : 1351 - 1352
  • [6] FACILE ALKYLATIVE CYCLIZATION - REGIOSELECTIVITY IN THE SYNTHESIS OF 2-METHYL-4H-THIENO[2,3-B][1]BENZOTHIOPYRAN-4-ONES AND THIOPYRANO[2,3-B][1]BENZOTHIOPYRAN-5-(4H)-ONES
    MAJUMDAR, KC
    SAHA, S
    KHAN, AT
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 1994, 33 (03): : 216 - 222
  • [7] SYNTHESIS AND SPECTRAL STUDIES OF 3-SUBSTITUTED-2H-PYRANO[2,3-B]QUINOLIN-2-ONES
    TILAKRAJ, T
    AMBEKAR, SY
    JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1986, 63 (11) : 981 - 983
  • [8] HETEROCYCLES STRUCTURALLY INFLUENCED BY A SIDE-CHAIN .7. 3-PHENACYLIDENE-3,4-DIHYDRO-1H-PYRIDO[2,3-B]PYRAZIN-2-ONES AND 2-PHENACYLIDENE-1,2-DIHYDRO-4H-PYRIDO[2,3-B]PYRAZIN-3-ONES
    SEKI, T
    SAKATA, H
    IWANAMI, Y
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 1995, 32 (01) : 347 - 348
  • [9] SYNTHESIS OF THIENO[2,3-B]AZEPIN-4-ONES
    KOEBEL, RF
    BLANTON, CD
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1973, : 54 - &
  • [10] Synthesis and cytotoxicity of novel 6H-indolo[2,3-b]quinoxaline derivatives
    Avula, Sreenivas
    Komsani, Jayaram Reddy
    Koppireddi, Satish
    Yadla, Rambabu
    Kanugula, Anantha KoteswaraRao
    Kotamraju, Srigiridhar
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (08) : 3712 - 3718