Design and synthesis of new pyrimidine derivatives clubbed with thiazolidin-4-one from 4-(2-chlorophenyl)-6-(2,4-dichlorophenyl)pyrimidin-2-amine and their in vitro anticancer activities were screened at National Cancer Institute (NCI), USA against full NCI 60 cell lines. Compound 2 (NSC: 765735) exhibited remarkable growth inhibition at single dose (10 mu M) and encourage chosen for broadcast at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 mu M). The compound 2 was found better quality for Lung cancer cell line (HOP-92) by viewing growth inhibition (GI(50) 0.52) and no cytotoxicity seen (LC50 > 100). Molecular docking study was performed using Maestro 9.0 (Schrodinger Inc. USA) to provide binding mode into binding sites of CDK2. Compound 2 could be used as a lead compound for developing new potential anticancer agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
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Grigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, RomaniaGrigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, Romania
Lupascu, Florentina Geanina
Dragostin, Oana Maria
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Grigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, RomaniaGrigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, Romania
Dragostin, Oana Maria
Foia, Liliana
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Grigore T Popa Univ Med & Pharm, Dept Biochem, Fac Dent, Iasi 700115, RomaniaGrigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, Romania
Foia, Liliana
Lupascu, Dan
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Grigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, RomaniaGrigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, Romania
Lupascu, Dan
Profire, Lenuta
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Grigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, RomaniaGrigore T Popa Univ Med & Pharm, Dept Pharmaceut Chem, Fac Pharm, Iasi 700115, Romania
机构:
Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei UniversityKey Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University
Chen H.
Guo Z.
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Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei UniversityKey Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University
Guo Z.
Yin Q.
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Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei UniversityKey Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University
Yin Q.
Duan X.
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Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei UniversityKey Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University
Duan X.
Gu Y.
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Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei UniversityKey Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University
Gu Y.
Li X.
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Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei UniversityKey Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University
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Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
D'Ascenzio, Melissa
Bizzarri, Bruna
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Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Bizzarri, Bruna
De Monte, Celeste
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Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
De Monte, Celeste
Carradori, Simone
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Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Carradori, Simone
Bolasco, Adriana
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Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Bolasco, Adriana
Secci, Daniela
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Univ Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Secci, Daniela
Rivanera, Daniela
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Univ Roma La Sapienza, Dept Publ Hlth & Infect Dis, I-00185 Rome, ItalyUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Rivanera, Daniela
Faulhaber, Nathan
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Johns Hopkins Univ, Sch Med, Stanley Div Dev Neurovirol, Baltimore, MD 21287 USAUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Faulhaber, Nathan
Bordon, Claudia
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Johns Hopkins Univ, Sch Med, Stanley Div Dev Neurovirol, Baltimore, MD 21287 USAUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
Bordon, Claudia
Jones-Brando, Lorraine
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Johns Hopkins Univ, Sch Med, Stanley Div Dev Neurovirol, Baltimore, MD 21287 USAUniv Roma La Sapienza, Dept Drug Chem & Technol, I-00185 Rome, Italy
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Veer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, IndiaVeer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, India
Abhale, Yogita K.
Shinde, Abhijit
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Savitribai Phule Pune Univ, SP Mandalis Sir Parashurambhau Coll, Post Grad Dept Chem, Tilak Rd, Pune 411030, Maharashtra, IndiaVeer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, India
Shinde, Abhijit
Shelke, Monika
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Savitribai Phule Pune Univ, SP Mandalis Sir Parashurambhau Coll, Post Grad Dept Chem, Tilak Rd, Pune 411030, Maharashtra, IndiaVeer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, India
Shelke, Monika
Nawale, Laxman
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Natl Chem Lab, Combi Chem Bio Resource Ctr, Pune 411008, Maharashtra, IndiaVeer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, India
Nawale, Laxman
Sarkar, Dhiman
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Natl Chem Lab, Combi Chem Bio Resource Ctr, Pune 411008, Maharashtra, IndiaVeer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, India
Sarkar, Dhiman
Mhaske, Pravin C.
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Savitribai Phule Pune Univ, SP Mandalis Sir Parashurambhau Coll, Post Grad Dept Chem, Tilak Rd, Pune 411030, Maharashtra, IndiaVeer Narmad South Gujarat Univ, Govt Coll, Dept Chem, Surat, Daman, India