Medicinal Chemistry Research
https://doi.org/10.1007/s00044-018-2236-3
MEDICINAL
CHEMISTR Y
RESEARCH
ORIGINAL RESEARCH
Design, synthesis and identification of novel substituted
isothiochromene analogs as potential antiviral and cytotoxic agents
Ameen A. Abu-Hashem
1,2
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Moustafa A. Gouda
3,4
●
Farid A. Badria
5
Received: 30 January 2018 / Accepted: 17 August 2018
© Springer Science+Business Media, LLC, part of Springer Nature 2018
Abstract
In this study, we present the synthesis of novel isothiochromenes, thiazolidonone, thiazinone, arylidines, triazoles, and
pyrimidinone compounds based on the starting material 3-amino- isothiochromene-4-carbonitrile 3. The chemical structures
were confirmed using spectroscopic methods and elemental analyses. These compounds were screened for their in vitro
antiviral and antitumor activities. Compounds 10a-c and 22a-b showed activity against herpes simplex virus-1 (HSV-1) and
human immunodeficiency virus-1 (HIV-1). Compounds 15 and 21a-b exhibited activity against various types of cancer cell
lines.
Graphical Abstract
Compounds 22a-b and 10a-c showed to be active against herpes simplex virus-1 (HSV-1) and virus-1 (HIV-1). Also, the
products 21a-b and 15 proved to a wide extent antitumor activity
Keywords Isothiochromenes
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Thiazolopyrimidines
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Thiazines
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1, 2, 3-triazine
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Triazolopyrimidines
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Pyrrolopyrimidines
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Antiviral
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Antitumor activity
* Ameen A. Abu-Hashem
aminaliabuhashem@yahoo.com
1
Photochemistry Department (Heterocyclic Unit), National
Research Centre, Dokki, Giza 12622, Egypt
2
Chemistry Departments, Faculty of Science, Jazan University,
Jazan 2097, Saudi Arabia
3
Department of Chemistry, Faculty of Science and Arts, Taibah
University, Ulla, Medina, Saudi Arabia
4
Department of Chemistry, Faculty of Science, Mansoura
University, Mansoura 35516, Egypt
5
Pharmacognosy Department, Faculty of Pharmacy, Mansoura
University, Mansoura 35516, Egypt
Electronic supplementary material The online version of this article
(https://doi.org/10.1007/s00044-018-2236-3) contains supplementary
material, which is available to authorized users.
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