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

[1]

Abadi AH, 2003, CHEM PHARM BULL, V51, P838

[2] Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX [J].

Abbate, F ;

Casini, A ;

Owa, T ;

Scozzafava, A ;

Supuran, CT .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (01) :217-223

[3] Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2thione derivatives with carbonic anhydrase inhibitory activity [J].

Abdel-Hamid, Mohammed K. ;

Abdel-Hafez, Atef A. ;

El-Koussi, Nawal A. ;

Mahfouz, Nadia M. ;

Innocenti, Alessio ;

Supuran, Claudlu T. .

BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (22) :6975-6984

[4] Novel 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives: Promising anticancer agents [J].

Aboraia, AS ;

Abdel-Rahman, HM ;

Mahfouz, NM ;

El-Gendy, MA .

BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (04) :1236-1246

[5] Antibacterial and antifungal activities of new pyrazolo[3,4-d]pyridazin derivatives [J].

Akbas, E ;

Berber, I .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2005, 40 (04) :401-405

[6]

Bakhite EA, 2002, B KOREAN CHEM SOC, V23, P1715

[7] PREPARATION AND ANTITUMOR ACTIVITY OF SOME SCHIFF BASES OF 2'-AMINO-4',5'-DICHLOROBENZENESULFONANILIDE AND 2'-AMINO-PARA-TOLUENESULFONANILIDE [J].

BILLMAN, JH ;

SCHMIDGALL, RL .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1970, 59 (08) :1191-+

[8] Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases [J].

Braña, MF ;

Cacho, M ;

García, ML ;

Mayoral, EP ;

López, B ;

de Pascual-Teresa, B ;

Ramos, A ;

Acero, N ;

Llinares, F ;

Muñoz-Mingarro, D ;

Lozach, O ;

Meijer, L .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (22) :6843-6854

[9] Imidazo[1,2-b]pyridazines:: a potent and selective class of cyclin-dependent kinase inhibitors [J].

Byth, KF ;

Cooper, N ;

Culshaw, JD ;

Heaton, DW ;

Oakes, SE ;

Minshull, CA ;

Norman, RA ;

Pauptit, RA ;

Tucker, JA ;

Breed, J ;

Pannifer, A ;

Rowsell, S ;

Stanway, JJ ;

Valentine, AL ;

Thomas, AP .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (09) :2249-2252

[10] HETEROATOM ANALOGS OF BEMORADAN - CHEMISTRY AND CARDIOTONIC ACTIVITY OF 1,4-BENZOTHIAZINYLPYRIDAZINONES [J].

COMBS, DW ;

RAMPULLA, MS ;

DEMERS, JP ;

FALOTICO, R ;

MOORE, JB .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (01) :172-176

← 1 2 3 4 5 6 →