Synthesis and biological evaluation of amide derivatives of 1,2,4-thiadiazole-thiazole-pyridine as anticancer agents

被引：3

作者：

Nalla, Somaiah ^{[1
]}

Pavani, Y. ^{[2
]}

Gollapudi, Ravi kumar ^{[3
]}

Poodari, Sumalatha ^{[3
]}

Mannam, Subbarao ^{[1
]}

机构：

[1] Acharya Nagarjuna Univ, Dept Chem, Guntur 522510, Andhra Pradesh, India

[2] PVP Siddhartha Inst Technol, Dept Freshman Engn, Vijayawada, Andhra Pradesh, India

[3] Govt Degree Coll Autonomous, Siddipet 502103, Telangana, India

来源：

CHEMICAL DATA COLLECTIONS | 2024年 / 49卷

关键词：

Cefozopram; 1,2,4-thiadiazole; Dasatinib; Thiazole and anticancer activity; 1,2,4-THIADIAZOLE; THIAZOLE; DESIGN;

D O I：

10.1016/j.cdc.2023.101108

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A new series of amide derivatives (10a-j) were designed and synthesized and their structures were confirmed by analytical data. Further, all these derivatives (10a-j) were examined for in vitro antitumor activity against four human cancer cell lines like MCF-7 (breast), A549 (lung), Col- 205 (colon) and A2780 (ovarian) by using of the MTT assay. All the derivatives (10a-j) were exhibited remarkable anticancer effects on four cell lines as compared with etoposide used as a positive control. The IC50 values range of tested compounds from 0.11 f 0.051 mu M to 7.42 f 5.89 mu M; whereas, positive control showed IC50 values ranges from 0.17 f 0.034 mu M to 3.34 f 0.152 mu M, respectively. Among these derivatives, four compounds 10a, 10b, 10c & 10d demonstrated more potent activities than the positive control.

引用

页数：8

共 25 条

[11]

2-6

[12] Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres [J].

Kohara, Y ;

Kubo, K ;

Imamiya, E ;

Wada, T ;

Inada, Y ;

Naka, T .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (26) :5228-5235

[13] Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective [J].

Kumar, Adarsh ;

Singh, Ankit Kumar ;

Singh, Harshwardhan ;

Vijayan, Veena ;

Kumar, Deepak ;

Naik, Jashwanth ;

Thareja, Suresh ;

Yadav, Jagat Pal ;

Pathak, Prateek ;

Grishina, Maria ;

Verma, Amita ;

Khalilullah, Habibullah ;

Jaremko, Mariusz ;

Emwas, Abdul-Hamid ;

Kumar, Pradeep .

PHARMACEUTICALS, 2023, 16 (02)

[14] Synthesis of 3-[4′-(p-chlorophenyl)-thiazol-2′-yl]-2-[(substituted azetidinone/thiazolidinone)-aminomethyl]-6-bromoquinazolin-4-ones as anti-inflammatory agent [J].

Kumar, Ashok ;

Rajput, Chatrasal Singh ;

Bhati, Sudhir Kumar .

BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (08) :3089-3096

[15] 1,2,4-thiadiazole: A novel Cathepsin B inhibitor [J].

Leung-Toung, R ;

Wodzinska, J ;

Li, WR ;

Lowrie, J ;

Kukreja, R ;

Desilets, D ;

Karimian, K ;

Tam, TF .

BIOORGANIC & MEDICINAL CHEMISTRY, 2003, 11 (24) :5529-5537

[16] Design, synthesis, and biological activity of novel 4-(3,4dimethoxyphenyl)-2-methylthiazole-5-carboxylic acid derivatives [J].

Liu, CL ;

Li, L ;

Li, ZM .

BIOORGANIC & MEDICINAL CHEMISTRY, 2004, 12 (11) :2825-2830

[17] An investigation of phenylthiazole antiflaviviral agents [J].

Mayhoub, Abdelrahman S. ;

Khaliq, Mansoora ;

Botting, Carolyn ;

Li, Ze ;

Kuhn, Richard J. ;

Cushman, Mark .

BIOORGANIC & MEDICINAL CHEMISTRY, 2011, 19 (12) :3845-3854

[18] Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality as Anticancer Agents [J].

Pragathi, Yazala Jyothsna ;

Sreenivasulu, Reddymasu ;

Veronica, Deekala ;

Raju, Rudraraju Ramesh .

ARABIAN JOURNAL FOR SCIENCE AND ENGINEERING, 2021, 46 (01) :225-232

[19] Hybrid molecules containing benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and α-bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukaemia cells [J].

Romagnoli, Romeo ;

Baraldi, Pier Giovanni ;

Carrion, Maria Dora ;

Cruz-Lopez, Olga ;

Preti, Delia ;

Tabrizi, Mojgan Aghazadeh ;

Fruttarolo, Francesca ;

Hellmann, Joerg ;

Bermejo, Jaime ;

Estevez, Francisco .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (10) :2844-2848

[20] Syntheses and evaluation of antioxidant activity of sydnonyl substituted thiazolidinone and thiazoline derivatives [J].

Shih, MH ;

Ke, FY .

BIOORGANIC & MEDICINAL CHEMISTRY, 2004, 12 (17) :4633-4643

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