Shaker Youssif

Zagazig University, Egypt

Title: Novel Pyran-Functionalized Uracil Derivatives: Design, Synthesis, Antitumor Activity and Docking Studies

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Biography

Abstract

Twelve novel pyran-based uracils were synthesized. 5-(Pyran-2-yl)uracil derivatives 3, starting with 5-acetyl-6-aminouracil (2). The reaction of compound 3 with reagents like ethyl cyanoacetate, urea, thiourea, hydrazine hydrate, formic acid, formamide, sulphuric acid, HCl/ AcOH, Ac2O, phenyl isocyanate, and carbon disulfide, respectively, afforded compounds 4-14 in good yields. The anticancer activity of the compounds was assessed using MTT and wound healing assays to detect their cytotoxicity, antiproliferative and antimigratory activities, respectively. Compounds 3, 5, 6, 7, 8, 9, 10, 11, and 13 significantly inhibited cell proliferation of hepatocellular carcinoma HepG2 cell line. Whereas, compounds 7, 8, 9 and 13 significantly inhibited the proliferation of ovarian cancer cell line SKOV3. The ability of synthesized compounds for induction of cell apoptosis and inhibition of cell migration was molecularly validated by the ability of 10 and 7 to inhibit the transcription of survivin and cluster of differentiation 44 (CD44) transcripts of HepG2 and SKOV3 cells, respectively