Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives

被引：25

作者：

Gurdal, Enise Ece ^{[1
]}

Buclulgan, Ebru ^{[1
]}

Durmaz, Irem ^{[2
]}

Cetin-Atalay, Rengul ^{[2
]}

Yarim, Mine ^{[1
]}

机构：

[1] Yeditepe Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34755 Istanbul, Turkey

[2] Bilkent Univ, Dept Mol Biol & Genet, Genet & Biotechnol Res Ctr, BilGen,Fac Sci, TR-06800 Ankara, Turkey

来源：

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY | 2015年 / 15卷 / 03期

关键词：

Anticancer; apoptosis; benzothiazole; cytotoxicity; piperazine; sulphorhodamine B; BIOLOGICAL EVALUATION; IN-VITRO; DESIGN;

D O I：

10.2174/1871520615666141216151101

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Aroyl substituted compounds 1h and 1j were found to be the most active derivatives. In addition, further investigation of compounds 1h and 1j by Hoechst staining and FACS revealed that these compounds cause apoptosis by cell cycle arrest at subG1 phase. HN

引用

页码：382 / 389

页数：8

共 35 条

[1] Synthesis and in vitro antiproliferative activity of new benzothiazole derivatives [J].

Al-Soud, Yaseen A. ;

Al-Sa'doni, Haitham H. ;

Saeed, Bahjat ;

Jaber, Ihsan H. ;

Beni-Khalid, Mohammad O. ;

Al-Masoudi, Najim A. ;

Abdul-Kadir, Tahsin ;

La Colla, Paolo ;

Busonera, Bernardetta ;

Sanna, Tiziana ;

Loddo, Roberta .

ARKIVOC, 2008, :225-238

[2] Synthesis, anticonvulsant activity and 3D-QSAR study of some prop-2-eneamido and 1-acetyl-pyrazolin derivatives of aminobenzothiazole [J].

Amnerkar, Nikhil D. ;

Bhusari, Kishore P. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (01) :149-159

[3] Effects of imatinib and interferon on primitive chronic myeloid leukaemia progenitors [J].

Angstreich, GR ;

Matsui, W ;

Huff, CA ;

Vala, MS ;

Barber, J ;

Hawkins, AL ;

Griffin, CA ;

Smith, GBD ;

Jones, RJ .

BRITISH JOURNAL OF HAEMATOLOGY, 2005, 130 (03) :373-381

[4]

[Anonymous], INT J PHARM SCI DRUG

[5]

[Anonymous], WHAT IS CANC

[6] Synthesis and antimicrobial activity of some new thiazole, thiophene and pyrazole derivatives containing benzothiazole moiety [J].

Bondock, Samir ;

Fadaly, Walid ;

Metwally, Mohamed A. .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (09) :3692-3701

[7]

Callery P, 2002, FOYES PRINCIPLES MED, P924

[8]

Choudhary S., 2013, PHARM CHEM, V5, P213

[9]

Devmurari V.P., 2010, INT J CHEM TECH RES, V2, P681

[10]

Gupta S, 2009, INDIAN J CHEM B, V48, P853

← 1 2 3 4 →