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Sulfonamide phenylalanine (SPA) series of analogues as an antibacterial, antifungal, anticancer agents along with p53 tumor suppressor-DNA complex inhibitor - part 1.

Authors
  • Devi, Kirna1
  • Awasthi, Pamita1
  • 1 Department of Chemistry, National Institute of Technology, Hamirpur, Himachal Pradesh, India. , (India)
Type
Published Article
Journal
Journal of biomolecular structure & dynamics
Publication Date
Sep 01, 2020
Volume
38
Issue
14
Pages
4081–4097
Identifiers
DOI: 10.1080/07391102.2019.1671229
PMID: 31547774
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

A series of N-[1-benzyl-2-oxo-2-substituted(ethyl)] benzene/p-toluene sulfonamide (K1-K12) are synthesized. Structure of the synthesized analogues has been confirmed by FT-IR, 1H & 13C NMR and ESI-MS spectroscopic techniques. All the synthesized analogues (K1-K12) have also been examined for their in-vitro antibacterial and antifungal activities. Compounds showed good antibacterial and antifungal activity against standard drug. Anticancer study has been carried out on three cancer cell lines PC-3, MCF-7 and A549 on two different concentrations (mg/mL and μg/mL). The K4 sulfonamide analogue showed better anticancer activity amongst all analogues against PC-3 and A549 cell lines. K4 inhibit G0/G1 phase in cell-cycle analysis experiment. All synthesized molecules (K1-K12) dock at junction p53-DNA and make hydrogen bonded with residues of p53 protein as per docking study. ADMET predictions of synthesized phenylalanine sulfonamide analogues (K1-K12) has been done using 'Lipinski rule' and it has been observed that all synthesized analogues did not violate the rule. Electronic, chemical properties and mulliken atomic charges of analogues were calculated using density functional theory (DFT). Communicated by Ramaswamy H. Sarma.

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