Synthesis and Antitumor Activity of Novel Arylpiperazine Derivatives Containing the Saccharin Moiety

被引：12

作者：

Chen, Hong ^{[1
]}

Xu, Bing-Bing ^{[2
]}

Sun, Tao ^{[1
]}

Zhou, Zhan ^{[1
]}

Ya, Hui-Yuan ^{[1
]}

Yuan, Mu ^{[2
]}

机构：

[1] Luoyang Normal Univ, Coll Food & Drug, 6 Jiqing Rd, Luoyang 471934, Peoples R China

[2] Guangzhou Med Univ, Pharmaceut Res Ctr, 195 Dongfengxi Rd, Guangzhou 511436, Guangdong, Peoples R China

来源：

MOLECULES | 2017年 / 22卷 / 11期

关键词：

synthesis; arylpiperazine derivatives; cytotoxic activity; CCK-8; structure-activity relationship; BENIGN PROSTATIC HYPERPLASIA; ACUTE LYMPHOBLASTIC-LEUKEMIA; CANCER CELL-LINES; ANDROGEN RECEPTOR; ALPHA(1)-ADRENOCEPTOR ANTAGONISTS; NAFTOPIDIL; INHIBITORS; MANAGEMENT; RESISTANCE; KINETICS;

D O I：

10.3390/molecules22111857

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Prostate cancer is a major public health problem worldwide. For the development of potential anti-prostate cancer agents, a series of novel arylpiperazine derivatives containing the saccharin moiety based on previous studies was designed, synthesized, and evaluated in prostate (PC-3, LNCaP, and DU145) cancer cell lines for their anticancer activities. The majority of the compounds exhibited excellent selective activity for the tested cancer cells. Compounds 4 and 12 exhibited strong cytotoxic activities against DU145 cells (half maximal inhibitory concentration (IC50) < 2 M). The structure-activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data. This work provides a potential lead compound for anticancer agent development focusing on prostate cancer therapy.

引用

页数：13

共 32 条

[1] Design and synthesis of D-ring steroidal isoxazolines and oxazolines as potential antiproliferative agents against LNCaP, PC-3 and DU-145 cells [J].

Banday, Abid H. ;

Giri, Aswini K. ;

Parveen, Rifat ;

Bashir, Nusrat .

STEROIDS, 2014, 87 :93-98

[2] Androgen receptors in prostate cancer [J].

Bentel, JM ;

Tilley, WD .

JOURNAL OF ENDOCRINOLOGY, 1996, 151 (01) :1-11

[3]

Chen H., 2015, MED CHEM LETT, V25, P285, DOI [10.1016/j.bmcl.2014.11.04925488843, DOI 10.1016/J.BMCL.2014.11.04925488843]

[4] Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines [J].

Chen, Hong ;

Xu, Fang ;

Xu, Bing-Bing ;

Xu, Jing-Yi ;

Shao, Bin-Hao ;

Huang, Bi-Yun ;

Yuan, Mu .

CHINESE CHEMICAL LETTERS, 2016, 27 (02) :277-282

[5] Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines [J].

Chen, Hong ;

Liang, Xue ;

Xu, Fang ;

Xu, Bingbing ;

He, Xuelan ;

Huang, Biyun ;

Yuan, Mu .

MOLECULES, 2014, 19 (08) :12048-12064

[6] 1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase [J].

Combrink, KD ;

Gülgeze, HB ;

Meanwell, NA ;

Pearce, BC ;

Pi, ZL ;

Bisacchi, GS ;

Roberts, DGM ;

Stanley, P ;

Seiler, SM .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (24) :4854-4860

[7] Androgen receptors in prostate cancer [J].

Culig, Z ;

Klocker, H ;

Bartsch, G ;

Hobisch, A .

[8]

DeFrancesco L, 2001, NAT MED, V7, P1076, DOI 10.1038/nm1001-1076a

[9] Androgen receptor structural and functional elements: Role and regulation in prostate cancer [J].

Dehm, Scott M. ;

Tindall, Donald J. .

MOLECULAR ENDOCRINOLOGY, 2007, 21 (12) :2855-2863

[10] Gain of miR-151 on chromosome 8q24.3 facilitates tumour cell migration and spreading through downregulating RhoGDIA [J].

Ding, Jie ;

Huang, Shenglin ;

Wu, Shunquan ;

Zhao, Yingjun ;

Liang, Linhui ;

Yan, Mingxia ;

Ge, Chao ;

Yao, Jian ;

Chen, Taoyang ;

Wan, Dafang ;

Wang, Hongyang ;

Gu, Jianren ;

Yao, Ming ;

Li, Jinjun ;

Tu, Hong ;

He, Xianghuo .

NATURE CELL BIOLOGY, 2010, 12 (04) :390-U208

← 1 2 3 4 →