Design and synthesis of some thieno[2,3-c]pyridazine derivatives of expected anticancer activity

被引：10

作者：

El-Ansary, Afaf K. ^{[1
]}

Kamal, Aliaa M. ^{[1
]}

Al-Ghorafi, Mokhtar AbdHafiz ^{[1
]}

机构：

[1] Cairo Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Cairo 11561, Egypt

来源：

MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 06期

关键词：

Antitumour agents; Thieno[2,3-c]pyridazines; Cytotoxic activity; Pharmacophores; Improving chemotherapy regimen; PYRIDAZINE DERIVATIVES; POTENTIAL ANTITUMOR; SCHIFF-BASES; AGENTS; SERIES; ACID; INHIBITORS; ANALOGS; THIOSEMICARBAZONE; ANTIBACTERIAL;

D O I：

10.1007/s00044-012-0258-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Design and synthesis of some new thienopyridazine derivatives as anticancer agents were the goal of this work. Accordingly, a series of novel compounds were synthesized via reacting thienopyridazine carboxylic acid hydrazide with different organic reagents. Twelve novel compounds were selected by National Cancer Institute for a full anticancer screening assay where seven of the investigated compounds showed non-selective broad spectrum and promising activity almost against all cancer cell lines. One of the most active compounds was chosen to be evaluated against 60-cell line panel at five concentration levels and revealed a remarkable growth inhibition activity.

引用

页码：2589 / 2601

页数：13

共 54 条

[31] A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models:: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners [J].

Mylari, BL ;

Armento, SJ ;

Beebe, DA ;

Conn, EL ;

Coutcher, JB ;

Dina, MS ;

O'Gorman, MT ;

Linhares, MC ;

Martin, WH ;

Oates, PJ ;

Tess, DA ;

Withbroe, GJ ;

Zembrowski, WJ .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (20) :6326-6339

[32] Synthesis of new series of 1-aryl-1,4-dihydro-4-oxo-6-methyl pyridazine-3-carboxylic acid as potential antibacterial agents [J].

Nagawade, RR ;

Khanna, VV ;

Bhagwat, SS ;

Shinde, DB .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2005, 40 (12) :1325-1330

[33] Discovery of novel antitumor sulfonamides targeting G1 phase of the cell cycle [J].

Owa, T ;

Yoshino, H ;

Okauchi, T ;

Yoshimatsu, K ;

Ozawa, Y ;

Sugi, NH ;

Nagasu, T ;

Koyanagi, N ;

Kitoh, K .

JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (19) :3789-3799

[34] CONFORMATIONAL BEHAVIOR AND E/Z ISOMERIZATION OF N-ACYL AND N-AROYLHYDRAZONES [J].

PALLA, G ;

PREDIERI, G ;

DOMIANO, P ;

VIGNALI, C ;

TURNER, W .

TETRAHEDRON, 1986, 42 (13) :3649-3654

[35] Local anti-inflammatory effect and behavioral studies on new PDE4 inhibitors [J].

Pieretti, Stefano ;

Dominici, Luigi ;

Di Giannuario, Amalia ;

Cesari, Nicoletta ;

Dal Piaz, Vittorio .

LIFE SCIENCES, 2006, 79 (08) :791-800

[36] SYNTHESIS AND ANTIHYPERTENSIVE PROPERTIES OF NEW 3-HYDRAZINOPYRIDAZINE DERIVATIVES [J].

PIFFERI, G ;

PARRAVICINI, F ;

CARPI, C ;

DORIGOTTI, L .

JOURNAL OF MEDICINAL CHEMISTRY, 1975, 18 (07) :741-746

[37] SYNTHESIS OF POTENTIAL ANTICANCER AGENTS .2. SOME SCHIFF BASES [J].

POPP, FD .

JOURNAL OF ORGANIC CHEMISTRY, 1961, 26 (05) :1566-&

[38] SYNTHESIS OF POTENTIAL ANTICANCER AGENTS .5. SCHIFF BASES AND RELATED COMPOUNDS [J].

POPP, FD ;

KIRSCH, W .

JOURNAL OF ORGANIC CHEMISTRY, 1961, 26 (10) :3858-&

[39] Novel tetranuclear orthometalated complexes of Pd(II) and Pt(II) derived from p-isopropylbenzaldehyde thiosemicarbazone with cytotoxic activity in cis-DDP resistant tumor cell lines.: Interaction of these complexes with DNA [J].

Quiroga, AG ;

Pérez, JM ;

López-Solera, I ;

Masaguer, JR ;

Luque, A ;

Román, P ;

Edwards, A ;

Alonso, C ;

Navarro-Ranninger, C .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (09) :1399-1408

[40] Synthesis of novel thieno[2,3-c]pyridazines and related heterocycles [J].

Radwan, SM ;

Bakhite, EA .

MONATSHEFTE FUR CHEMIE, 1999, 130 (09) :1117-1128

← 1 2 3 4 5 6 →