Synthesis, characterization, crystal structures and biological screening of 4-amino quinazoline sulfonamide derivatives
Kumar, A. S., Kudva, J., Lahtinen, M., Peuronen, A., Sadashiva, R., & Naral, D. (2019). Synthesis, characterization, crystal structures and biological screening of 4-amino quinazoline sulfonamide derivatives. Journal of Molecular Structure, 1190, 29-36. https://doi.org/10.1016/j.molstruc.2019.04.050
Published inJournal of Molecular Structure
©2019 Published by Elsevier B.V.
Three quinazolin-4-ylamino derivatives containing phenylbenzenesulfonamides (7a-7c) were synthesized by reacting (E)-N'-(2-cyanophenyl)-N,N-dimethyl formamidine (6) with different 4- amino-N-(phenyl)benzenesulfonamides (4a-4c) and characterized by different techniques such as HRMS, IR, 1H NMR and 13C NMR spectroscopy. The structural properties were further examined by single crystal X-ray diffraction method. The X-ray data shows that compounds 7a and 7c contain two molecules and 7b contains one molecule in the asymmetric unit. Comparison of conformation of two distinct molecules, “A” and “B”, in the asymmetric unit of 7a and 7c were studied with the aid of reported literature. The in vitro antiproliferative activity of the compounds was tested against two breast cancer cell lines (MDA-MB-231 and MCF7). Compound 7b observed as a highest potent candidate against MDA-MB-231with IC50 of 5.44 µg/mL. Antimicrobial activity was also screened against bacterial and fungal strains. Compound 7a with chloro substitution was observed as the most potent candidate against the Gram-negative bacterial strains, whereas the compounds showed no significant activity against the fungal strain. ...
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Related funder(s)Academy of Finland
Funding program(s)Academy Project, AoF
Additional information about fundingThe authors are gratefully acknowledge the financial support provided by VGST-K-FIST (L1)/2017, GRD No. 557 and the Academy of Finland (Project No. 277250 and 315911).
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