Synthesis and Cytotoxic Activity of New Thiazolopyrimidine Sugar Hydrazones and Their Derived Acyclic Nucleoside Analogues

New thienyl- or chlorophenyl-substituted thiazolopyrimidine derivatives and their derived sugar hydrazones incorporating acyclic <span style="font-variant: small-caps;">d</span>-galactosyl or <span style="font-variant: small-caps;">d</span>-xylosyl sugar m...

Full description

Bibliographic Details
Main Authors: Ebtesam A. Basiony, Allam A. Hassan, Zahra M. Al-Amshany, Ahmed A. Abd-Rabou, Adel A.-H. Abdel-Rahman, Nasser A. Hassan, Wael A. El-Sayed
Format: Article
Language:English
Published: MDPI AG 2020-01-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/25/2/399
Description
Summary:New thienyl- or chlorophenyl-substituted thiazolopyrimidine derivatives and their derived sugar hydrazones incorporating acyclic <span style="font-variant: small-caps;">d</span>-galactosyl or <span style="font-variant: small-caps;">d</span>-xylosyl sugar moieties in addition to their per-O-acetylated derivatives were synthesized. Heterocyclization of the formed sugar hydrazones afforded the derived acyclic nucleoside analogues possessing the 1,3,4-oxadiazoline as modified nucleobase via acetylation followed by the cyclization process. The cytotoxic activity of the synthesized compounds was studied against human breast cancer MCF7 and MDA-MB-231 cell lines as well as human colorectal cancer HCT 116 and Caco-2 cell lines. High activities were revealed by compounds <b>1</b>, <b>8</b>, <b>10</b>, <b>11</b>, and <b>13</b> against Caco-2 and MCF7 cells in addition to moderate activities exhibited by other compounds against HCT116 or MDA-MB-231 cells.
ISSN:1420-3049