Synthesis of novel S-acyl and S-alkylpyrimidinone derivatives as potential cytotoxic agents

Synthesis of novel S-acyl and S-alkylpyrimidinone derivatives as potential cytotoxic agents Makaram M. Said, Azza T. Taher, Hala B. El-Nassan , Eman A. El-Khouly Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt New S-acyl and S-alkylpyrimidinones were synthesized as cytotoxic agents. Compound 8g was the most potent cytotoxic on MCF-7 cell line. Compound 8g was potent and selective pim1 inhibitor. N O O N S 8g Cl Keywords Pyrimidine  Antitumor activity  MCF-7  HCT-116  pim1 Introduction Cancer is considered the second leading cause of death worldwide after cardiovascular diseases [1]. In spite of the presence of a large number of chemotherapeutic agents, they cause severe side effects and development of resistance by cancer cells even against drugs developed by targeted therapy such as imitanib [2]. Therefore, there is a continuous need for the development of novel molecules that can overcome cellular resistance. Since the introduction of 5-flourouracil in the late 1950s as a potent anticancer agent, many uracil and thiouracil derivatives have been reported as cytotoxic agents [3]. In addition, 4-aryl-5-cyanopyrimidinone derivatives were recently reported as cytotoxic agents [4–7]. In most of these derivatives, alkylation of the 2-thio group especially with alkylamino or acetanilide moieties (such as compounds I–IV, Fig. 1) was reported http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Synthesis of novel S-acyl and S-alkylpyrimidinone derivatives as potential cytotoxic agents

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Publisher
Springer Journals
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2487-x
Publisher site
See Article on Publisher Site

Abstract

Makaram M. Said, Azza T. Taher, Hala B. El-Nassan , Eman A. El-Khouly Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt New S-acyl and S-alkylpyrimidinones were synthesized as cytotoxic agents. Compound 8g was the most potent cytotoxic on MCF-7 cell line. Compound 8g was potent and selective pim1 inhibitor. N O O N S 8g Cl Keywords Pyrimidine  Antitumor activity  MCF-7  HCT-116  pim1 Introduction Cancer is considered the second leading cause of death worldwide after cardiovascular diseases [1]. In spite of the presence of a large number of chemotherapeutic agents, they cause severe side effects and development of resistance by cancer cells even against drugs developed by targeted therapy such as imitanib [2]. Therefore, there is a continuous need for the development of novel molecules that can overcome cellular resistance. Since the introduction of 5-flourouracil in the late 1950s as a potent anticancer agent, many uracil and thiouracil derivatives have been reported as cytotoxic agents [3]. In addition, 4-aryl-5-cyanopyrimidinone derivatives were recently reported as cytotoxic agents [4–7]. In most of these derivatives, alkylation of the 2-thio group especially with alkylamino or acetanilide moieties (such as compounds I–IV, Fig. 1) was reported

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Mar 11, 2016

References

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