Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Design and synthesis of new energy restriction mimetic agents: Potent anti-tumor activities of hybrid motifs of aminothiazoles and coumarins

(2020) Fatema Hersi et al.   Scientific Reports

New thiazol-hydrazono-coumarin hybrids targeting human cervical cancer cells: Synthesis, CDK2 inhibition, QSAR and molecular docking studies

(2019) Somaia S. Abd El-Karim et al.   BIOORGANIC CHEMISTRY

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action

(2019) Benoît Bestgen et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site

(2019) Benoît Bestgen et al.   JOURNAL OF MEDICINAL CHEMISTRY

2‐Amino‐5‐arylazothiazole‐Based Derivatives: In Vitro Cytotoxicity, Antioxidant Properties, and Bleomycin‐Dependent DNA Damage

(2019) Khalid M. Al‐Anazi et al.   ChemistrySelect

Immune checkpoint inhibitors: a promising anticancer therapy

(2019) Sima Singh et al.   DRUG DISCOVERY TODAY

Synthesis and biological evaluation of triterpenoid thiazoles derived from betulonic acid, dihydrobetulonic acid, and ursonic acid

(2019) Lucie Borková et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thiazole-containing compounds as therapeutic targets for cancer therapy

(2019) Prabodh Chander Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of 4β-(thiazol-2-yl)amino-4′- O -demethyl-4-deoxypodophyllotoxins as topoisomerase-II inhibitors

(2018) Chun-Yan Sang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of 4-amino-5-cinnamoylthiazoles as chalcone-like anticancer agents

(2018) Adileh Ayati et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of new coumarins bearing 2,4-diaminothiazole-5-carbonyl moiety

(2018) Adileh Ayati et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of 2-Aminothiazole Derivatives in Easy Two-Step, One-Pot Reaction

(2018) Błażej Dziuk et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Latest Research on Synthetics Compounds with Antileishmanial Activity

(2018) Carlos H. Rios Martinez et al.   MINI-REVIEWS IN ORGANIC CHEMISTRY

Design, Synthesis, and Evaluation of a New Series of Thiazole-Based Anticancer Agents as Potent Akt Inhibitors

(2018) Mehlika Altıntop et al.   MOLECULES

Alpelisib Plus Fulvestrant in PIK3CA-Altered and PIK3CA-Wild-Type Estrogen Receptor–Positive Advanced Breast Cancer

(2018) Dejan Juric et al.   JAMA Oncology

Enriching biologically relevant chemical space around 2-aminothiazole template for anticancer drug development

(2017) Sarah Titus et al.   MEDICINAL CHEMISTRY RESEARCH

Synthesis and antitumor activity of novel N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)-2-(piperazin-1-yl)acetamides

(2017) Zhilin Wu et al.   RESEARCH ON CHEMICAL INTERMEDIATES

Synthesis and bioevaluation of N,4-diaryl-1,3-thiazole-2-amines as tubulin inhibitors with potent antiproliferative activity

(2017) Maolin Sun et al.   PLoS One

Small Molecule TH-39 Potentially Targets Hec1/Nek2 Interaction and Exhibits Antitumor Efficacy in K562 Cells via G0/G1 Cell Cycle Arrest and Apoptosis Induction

(2016) Yongxia Zhu et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives

(2016) Hongshuang Li et al.   CHEMICAL RESEARCH IN CHINESE UNIVERSITIES

Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity

(2016) Yong-Hak Kim et al.   ChemMedChem

Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold

(2016) Lin Li et al.   CHINESE CHEMICAL LETTERS

1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation

(2016) Sahar M. Abou-Seri et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells

(2016) Antoine Millet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure–Activity Relationship Study

(2016) Matthias Schiedel et al.   JOURNAL OF MEDICINAL CHEMISTRY

From Sphingosine Kinase to Dihydroceramide Desaturase: A Structure–Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-Chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II)

(2016) Luigi Aurelio et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents

(2016) Chia-Ying Tsai et al.   MOLECULES

A Simple and Efficient Method for the Synthesis of 2-Aminothiazoles Under Mild Conditions

(2016) Z. Abedi-Jazini et al.   POLYCYCLIC AROMATIC COMPOUNDS

Synthesis and antiproliferative activity of D-ring substituted steroidal benzamidothiazoles

(2016) Ning-Juan Fan et al.   STEROIDS

Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma

(2016) S. K. Saha et al.   Cancer Discovery

Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors

(2016) Xin Chen et al.   RSC Advances

Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity

(2015) Xiao-Xiao Xie et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of benzothiazole-6-sulfonamides acting as highly potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII

(2015) Diaa A. Ibrahim et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors

(2015) Robin A. Fairhurst et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors

(2015) Cinzia Maria Francini et al.   ChemMedChem

Synthesis of 2-aminothiazole derivatives from easily available thiourea and alkyl/aryl ketones using aqueous NaICl2

(2015) Shrikant M. Ghodse et al.   TETRAHEDRON LETTERS

Improved Angiostatic Activity of Dasatinib by Modulation with Hydrophobic Chains

(2015) Emilia Păunescu et al.   ACS Medicinal Chemistry Letters

Design, synthesis and evaluation of 2-aminothiazole derivatives as sphingosine kinase inhibitors

(2014) Dominik Vogt et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Farnesyltransferase inhibitors: CAAX mimetics based on different biaryl scaffolds

(2014) Valentina Straniero et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors

(2014) Zhiqing Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Benzothiazoles exhibit broad-spectrum antitumor activity: Their potency, structure–activity and structure–metabolism relationships

(2014) Xilei Xie et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Bifunctional ethyl 2-amino-4-methylthiazole-5-carboxylate derivatives: Synthesis and in vitro biological evaluation as antimicrobial and anticancer agents

(2014) Sherif A.F. Rostom et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Some New Benzimidazole-Thiazole Derivatives as Anticancer Agents

(2014) Zienab M. Nofal et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Discovery of 4-Aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 Inhibitors. Part I: Optimization of in Vitro Potencies and Pharmacokinetic Properties

(2014) Ying-Shuan E. Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and in Vitro Evaluation of New Nitro-Substituted Thiazolyl Hydrazone Derivatives as Anticandidal and Anticancer Agents

(2014) Mehlika Altıntop et al.   MOLECULES

Targeting tumour-supportive cellular machineries in anticancer drug development

(2014) Matthias Dobbelstein et al.   NATURE REVIEWS DRUG DISCOVERY

Aurora Kinases as Druggable Targets in Pediatric Leukemia: Heterogeneity in Target Modulation Activities and Cytotoxicity by Diverse Novel Therapeutic Agents

(2014) Aarthi Jayanthan et al.   PLoS One

A Novel Aminothiazole KY-05009 with Potential to Inhibit Traf2- and Nck-Interacting Kinase (TNIK) Attenuates TGF-β1-Mediated Epithelial-to-Mesenchymal Transition in Human Lung Adenocarcinoma A549 Cells

(2014) Jiyeon Kim et al.   PLoS One

Structure guided design of a series of sphingosine kinase (SphK) inhibitors

(2013) Darin J. Gustin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and antitumor activity of 4-tert-butyl-5-benzyl-2-benzyliminothiazoles

(2013) Jiao Ye et al.   CHEMICAL RESEARCH IN CHINESE UNIVERSITIES

4-Bromo-2-(piperidin-1-yl)thiazol-5-yl-phenyl methanone (12b) inhibits Na+/K+-ATPase and Ras oncogene activity in cancer cells

(2013) Florence Lefranc et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel acetamidothiazole derivatives: Synthesis and in vitro anticancer evaluation

(2013) Ahmed R. Ali et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel Nitrogen-Enriched Oridonin Analogues with Thiazole-Fused A-Ring: Protecting Group-Free Synthesis, Enhanced Anticancer Profile, and Improved Aqueous Solubility

(2013) Chunyong Ding et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases

(2013) Ernst Schonbrunn et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Benzothiazole/thiazole-Containing Hydroxamic Acids as Potent Histone Deacetylase Inhibitors and Antitumor Agents

(2013) Truong Tung et al.   Medicinal Chemistry

Sphingosine Kinase Activity Is Not Required for Tumor Cell Viability

(2013) Karen Rex et al.   PLoS One

Synthesis and biological evaluation of 2-substituted-4-(3′,4′,5′-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents

(2012) Romeo Romagnoli et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Multicomponent One-Pot Synthesis of Substituted Hantzsch Thiazole Derivatives Under Solvent Free Conditions

(2012) Bhaskar S. Dawane et al.   E-Journal of Chemistry

Substituted thiazoles VI. Synthesis and antitumor activity of new 2-acetamido- and 2 or 3-propanamido-thiazole analogs

(2012) Shahenda M. El-Messery et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Activities of 2-Amino-thiazole-5-carboxylic Acid Phenylamide Derivatives

(2011) Wukun Liu et al.   ARCHIV DER PHARMAZIE

Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase

(2011) Cristiano Bolchi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Convergent Synthesis and Biological Evaluation of 2-Amino-4-(3′,4′,5′-trimethoxyphenyl)-5-aryl Thiazoles as Microtubule Targeting Agents

(2011) Romeo Romagnoli et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Aminothiazoles as Therapeutic Leads for Prion Diseases

(2011) Alejandra Gallardo-Godoy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and anticancer evaluation of thiazolyl–chalcones

(2010) Hai-Bo Shi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Phase 1 pharmacokinetic and drug-interaction study of dasatinib in patients with advanced solid tumors

(2010) Faye M. Johnson et al.   CANCER

Synthesis and antitumor activity of ureas containing pyrimidinyl group

(2010) Chuanfei Jin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of CKD-516: A Potent Tubulin Polymerization Inhibitor with Marked Antitumor Activity against Murine and Human Solid Tumors

(2010) Jaekwang Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, anticonvulsant and toxicity screening of thiazolyl–thiadiazole derivatives

(2010) Nadeem Siddiqui et al.   MEDICINAL CHEMISTRY RESEARCH

Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators

(2009) Tomoharu Iino et al.   BIOORGANIC & MEDICINAL CHEMISTRY

SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples

(2009) Andrew Conroy et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Synthesis and identification of a new class of (S)-2,6-diamino-4,5,6,7-tetrahydrobenzo[d]thiazole derivatives as potent antileukemic agents

(2009) D. S. Prasanna et al.   INVESTIGATIONAL NEW DRUGS

Discovery of 2-Aminothiazoles as Potent Antiprion Compounds

(2009) S. Ghaemmaghami et al.   JOURNAL OF VIROLOGY

Synthesis and Anticancer Activities of Some Thiazole Derivatives

(2009) Ismail Kayagil et al.   PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS

Design, synthesis and characterization of novel 2-(2,4-disubstituted-thiazole-5-yl)-3-aryl-3H-quinazoline-4-one derivatives as inhibitors of NF-κB and AP-1 mediated transcription activation and as potential anti-inflammatory agents

(2008) Rajan S. Giri et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY