Design, Synthesis and Therapeutic Potential of Some 6, 6'-(1,4- phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine)analogues
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Published:2019-03-28
Issue:7
Volume:19
Page:609-621
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ISSN:1389-5575
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Container-title:Mini-Reviews in Medicinal Chemistry
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language:en
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Short-container-title:MRMC
Author:
Kumar Sanjiv1, Narasimhan Balasubramanian1, Lim Siong Meng2, Ramasamy Kalavathy2, Mani Vasudevan3, Shah Syed Adnan Ali2
Affiliation:
1. Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak-124001, India 2. Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia 3. Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Buraidah 51452, Saudi Arabia
Abstract
<P>Background: A series of 6, 6'-(1,4-phenylene)bis(4-(4-bromophenyl)pyrimidin-2-amine)
derivatives has been synthesized by Claisen-Schmidt condensation and its chemical structures was
confirmed by FT-IR, 1H/13C-NMR spectral and elemental analyses. The molecular docking study was
carried out to find the interaction between active bis-pyrimidine compounds with CDK-8 protein. The
in vitro antimicrobial potential of the synthesized compounds was determined against Gram-positive
and Gram-negative bacterial species as well fungal species by tube dilution technique. Antimicrobial
results indicated that compound 11y was found to be most potent one against E. coli (MICec = 0.67
µmol/mL) and C. albicans (MICca = 0.17 µmol/mL) and its activity was comparable to norfloxacin
(MIC = 0.47 µmol/mL) and fluconazole (MIC = 0.50 µmol/mL), respectively.
Conclusion:
Anticancer screening of the synthesized compounds using Sulforhodamine B (SRB) assay
demonstrated that compounds 2y (IC50 = 0.01 µmol/mL) and 4y (IC50= 0.02 µmol/mL) have high antiproliferative
potential against human colorectal carcinoma cancer cell line than the reference drug (5-
fluorouracil) and these compounds also showed best dock score with better potency within the ATP
binding pocket and may also be used lead for rational drug designing.</P>
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology,General Medicine
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