Design, synthesis and evaluation of small molecule imidazo[2,1-b][1,3,4]thiadiazoles as inhibitors of transforming growth factor-ß type-I receptor kinase (ALK5).

Patel, Harun M; Sing, Baljeet; Bhardwaj, Varun; Palkar, Mahesh; Shaikh, Mahamadhanif S; Rane, Rajesh; Alwan, Wesam S; Gadad, Andanappa K; Noolvi, Malleshappa N; Karpoormath, Rajshekhar

Patel, Harun M; Sing, Baljeet; Bhardwaj, Varun; Palkar, Mahesh; Shaikh, Mahamadhanif S; Rane, Rajesh; Alwan, Wesam S; Gadad, Andanappa K; Noolvi, Malleshappa N; Karpoormath, Rajshekhar.

Afiliação

Patel HM; Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa.
Sing B; Department of Pharmaceutical Chemistry, ASBASJSM College of Pharmacy, Bela (Ropar) 140111, Punjab, India.
Bhardwaj V; Department of Biotechnology, Bioinformatics and Pharmacy, Jaypee University of Information Technology, Waknaghat, Solan 173234, Himachal Pradesh, India.
Palkar M; Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa.
Shaikh MS; Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa.
Rane R; Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa.
Alwan WS; Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa.
Gadad AK; School Pharmacy, Faculty of Medical Sciences, EWMS Complex, Mt. Hope, The University of the West Indies, Trinidad and Tobago, West Indies.
Noolvi MN; Department of Pharmaceutical Chemistry, Shree Dhanvantary Pharmacy College, Kim (Surat) 3941110, Gujarat, India. Electronic address: mallesh7301@rediffmail.com.
Karpoormath R; Department of Pharmaceutical Chemistry, College of Health Sciences, University of KwaZulu-Natal (Westville Campus), Private Bag X54001, Durban 4000, South Africa. Electronic address: karpoormath@ukzn.ac.za.

Eur J Med Chem ; 93: 599-613, 2015 Mar 26.

Article em En | MEDLINE | ID: mdl-25234355

Assuntos

Desenho de Fármacos; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/farmacologia; Proteínas Serina-Treonina Quinases/antagonistas & inibidores; Receptores de Fatores de Crescimento Transformadores beta/antagonistas & inibidores; Tiadiazóis/síntese química; Tiadiazóis/farmacologia; Células CACO-2; Técnicas de Química Sintética; Humanos; Modelos Moleculares; Conformação Proteica; Inibidores de Proteínas Quinases/química; Proteínas Serina-Treonina Quinases/química; Receptor do Fator de Crescimento Transformador beta Tipo I; Receptores de Fatores de Crescimento Transformadores beta/química; Tiadiazóis/química

Palavras-chave

ALK5; Lipinski's rule; Synthesis imidazo [2,1-b][1,3,4]thiadiazole; XP docking

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiadiazóis / Desenho de Fármacos / Proteínas Serina-Treonina Quinases / Receptores de Fatores de Crescimento Transformadores beta / Inibidores de Proteínas Quinases Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2015 Tipo de documento: Article País de afiliação: África do Sul

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