Drug Res (Stuttg) 2013; 63(04): 210-215
DOI: 10.1055/s-0033-1337929
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Design, Synthesis and Biological Evaluation Studies of Novel Quinazoline Derivatives as Cytotoxic Agents

M. F. Zayed
1   Department of Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al-Madinah Al-munawarah, Kingdom of Saudi Arabia
2   Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
M. H. Hassan
3   Department of Pharmacology and Toxicology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
4   Department of Pharmacy, College of Medical Rehabilitation Sciences, Taibah University, Al-Madinah Al-munawarah, Kingdom of Saudi Arabia
› Author Affiliations
Further Information

Publication History

received 05 January 2013

accepted 13 February 2013

Publication Date:
13 March 2013 (online)


Some novel quinazoline derivatives 6a-h were designed, synthesized and evaluated for their in vitro cytotoxic activity against lymphoma cell line compared to etoposide as a reference drug. Compounds (S)-2-(6,8-diiodo-2-phenylquinazolin-4-ylamino)-3-phenylpropanoic acid (6 f), (S)-2-(6,8-diiodo-2-phenylquinazolin-4-ylamino)-3-(1H-imidazol-4-yl)propanoic acid (6 g) and (S)-2-(6,8-diiodo-2-phenylquinazolin-4-ylamino)-3-(1H-indol-3-yl) propanoic acid (6 h) had comparable higher cytotoxic activity than the reference drug. Compound 6 f, the most active compound, had IC50=13.2 µM. In an attempt to interpret such anti-cancer activity of these derivatives, their anti-inflammatory action was examined using the carrageenan induced rat paw edema method. The most active compounds showed moderate anti-inflammatory activity compared to the reference drug. In order to identify the most relevant physicochemical features important for high antitumor activity of the target compounds, specific 2D descriptors were calculated and correlated with the antileukemic activity.

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