New Pyrano[2,3-d:6,5-d']dipyrimidine Derivatives-Synthesis, in vitro Cytotoxicity and Computational Studies

Author(s): Suresh Maddila, Kovashnee Naicker, Sridevi Gorle, Surjyakant Rana, Kotaiah Yalagala, Surya N. Maddila, Moganavelli Singh, Parvesh Singh, Sreekantha B. Jonnalagadda.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 8 , 2016

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Abstract:

A new series of pyrano[2,3-d:6,5-d']dipyrimidine derivatives were synthesized and evaluated for their in vitro anticancer activity. The structures of all the synthesized compounds were confirmed by 1H NMR, 13C NMR, 15N NMR, HR-MS and FT-IR spectral analyses. The cytotoxic activities of these compounds against four human cancer (HeLa, SKBR-3, HepG2, and Caco-2) cell lines were determined. The synthesized compounds showed high selectivity, and four compounds (5e, 5f, 5g and 5i) showed excellent potent cytotoxicity against HeLa, SKBR-3, and HepG2 cancer cell lines. Furthermore, four other compounds (5a, 5c, 5b and 5d) have exhibited significant cytotoxicity activity in the SKBR-3 and HepG2 cell lines respectively, with moderate cytotoxicity seen in the HeLa cell line. Additionally, a molecular docking study was conducted to predict the anti-cancer behavior of the synthesized compounds via inhibition of the allosteric site of Human Kinesin Eg5.

Keywords: Synthesis, pyrimidines, pyranes, cytotoxicity activity, HeLa, SKBR-3, HepG2.

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Article Details

VOLUME: 16
ISSUE: 8
Year: 2016
Page: [1031 - 1037]
Pages: 7
DOI: 10.2174/1871520616666151123095932
Price: $58

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