Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 12, Pages 5576-5584Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.09.007
Keywords
Acylhydrazone; Synthesis; Antitumor activity; Configurational isomer; Toxicity
Categories
Funding
- National Key Project for Basic Research [2010CB126104]
- National High Technology Research and Development Program of China [2006AA10A201]
- Scientific Research Foundation of the Graduate School of China Agricultural University
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A pair of chemical isomeric structures of N-acylhydrazone compounds I and II were designed and synthesized. The reaction was carried out with high diastereoselectivity to obtain one configurational isomer in excellent yields. The exact configuration and conformation of IIa and IIe were confirmed by the X-ray single crystal diffraction. The antitumor bioassay revealed that some compounds exhibited excellent activity against the selected cancer cell lines. In particular, IIf (IC50 =16.4 mu M) was better than doxorubicin (IC50=53.3 mu M) against human promyelocytic leukemic cells (HL-60). Their toxicities were predicted in silico. The results showed that compounds II were safe and eligible to be development candidates. IIf showed great promise as a novel lead compound for further anticancer discovery. (C) 2010 Elsevier Masson SAS. All rights reserved.
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