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Maddila S, Naicker K, Gorle S, et al. New Pyrano[2,3-d:6,5-d']dipyrimidine Derivatives-Synthesis, in vitro Cytotoxicity and Computational Studies. Anticancer Agents Med Chem. 2016;16(8):1031-1037doi: 10.2174/1871520616666151123095932.
Maddila, S., Naicker, K., Gorle, S., Rana, S., Yalagala, K., Maddila, S. N., Singh, M., Singh, P., & Jonnalagadda, S. B. (2016). New Pyrano[2,3-d:6,5-d']dipyrimidine Derivatives-Synthesis, in vitro Cytotoxicity and Computational Studies. Anti-cancer agents in medicinal chemistry, 16(8), 1031-1037. https://doi.org/10.2174/1871520616666151123095932
Maddila, Suresh, et al. "New Pyrano[2,3-d:6,5-d']dipyrimidine Derivatives-Synthesis, in vitro Cytotoxicity and Computational Studies." Anti-cancer agents in medicinal chemistry vol. 16,8 (2016): 1031-1037. doi: https://doi.org/10.2174/1871520616666151123095932
Maddila S, Naicker K, Gorle S, Rana S, Yalagala K, Maddila SN, Singh M, Singh P, Jonnalagadda SB. New Pyrano[2,3-d:6,5-d']dipyrimidine Derivatives-Synthesis, in vitro Cytotoxicity and Computational Studies. Anticancer Agents Med Chem. 2016;16(8):1031-1037. doi: 10.2174/1871520616666151123095932. PMID: 26592746.
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Anticancer Agents Med Chem. 2016;16(8):1031-1037. doi: 10.2174/1871520616666151123095932.

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

Anti-cancer agents in medicinal chemistry

Suresh Maddila, Kovashnee Naicker, Sridevi Gorle, Surjyakant Rana, Kotaiah Yalagala, Surya N Maddila, Moganavelli Singh, Parvesh Singh, Sreekantha B Jonnalagadda

Affiliations

  1. Department of Chemistry, School of Chemistry & Physics, University of KwaZulu-Natal, Westville Campus, Chiltern Hills, Durban-4000, South Africa.

PMID: 26592746 DOI: 10.2174/1871520616666151123095932

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.

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

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