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Molecules 2016, 21(11), 1447; doi:10.3390/molecules21111447

Synthesis and Biological Evaluation of Novel 4-Morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine Derivatives Bearing Phenylpyridine/ Phenylpyrimidine-Carboxamides

1
School of Perfume and Aroma Technology, Shanghai Institute of Technology, Shanghai 201418, China
2
School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, China
3
Pharmacy Department, The Affiliated Hospital of Chongqing Three Gorges Medical College, Chongqing 404000, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 27 September 2016 / Revised: 24 October 2016 / Accepted: 26 October 2016 / Published: 31 October 2016
(This article belongs to the Section Organic Synthesis)
View Full-Text   |   Download PDF [2255 KB, uploaded 31 October 2016]   |  

Abstract

Four series of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives 11aj, 12aj, 13ag and 14ag bearing phenylpyridine/phenylpyrimidine- carboxamide scaffolds were designed, synthesized and their IC50 values against three cancer cell lines (A549, PC-3 and MCF-7) were evaluated. Eleven of the compounds showed moderate cytotoxicity activity against the cancer cell lines. Structure-activity relationships (SARs) and pharmacological results indicated that the introduction of phenylpyridine-carboxamide scaffold was beneficial for the activity. What’s more, the oxidation of the sulfur atom in thiopyran and various types of substituents on the aryl group have different impacts on different series of compounds. Furthermore, the positions of aryl group substituents have a slight impact on the activity of the phenylpyridine-carboxamide series compounds. View Full-Text
Keywords: thiopyrano[4,3-d]pyrimidine; phenylpyridine/phenylpyrimidine carboxamides; synthesis; cytotoxicity activity; PI3Kα kinase thiopyrano[4,3-d]pyrimidine; phenylpyridine/phenylpyrimidine carboxamides; synthesis; cytotoxicity activity; PI3Kα kinase
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Liu, H.; Wang, W.; Sun, C.; Wang, C.; Zhu, W.; Zheng, P. Synthesis and Biological Evaluation of Novel 4-Morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine Derivatives Bearing Phenylpyridine/ Phenylpyrimidine-Carboxamides. Molecules 2016, 21, 1447.

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