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Samir M. El-Moghazy, Nahed M. Eid, Sahar M. Abou-Seri and Shaimaa M. Abdel-Rahman *

SYNTHESIS AND IN VITRO ANTITUMOR ACTIVITY OF NEW 5-FURANOISOXAZOLINE AND 5-FURANOPYRAZOLINE DERIVATIVES. Samir M. El-Moghazy, Nahed M. Eid, Sahar M. Abou-Seri and Shaimaa M. Abdel-Rahman * Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University.

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Samir M. El-Moghazy, Nahed M. Eid, Sahar M. Abou-Seri and Shaimaa M. Abdel-Rahman *

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  1. SYNTHESIS AND IN VITRO ANTITUMOR ACTIVITY OF NEW 5-FURANOISOXAZOLINE AND 5-FURANOPYRAZOLINE DERIVATIVES Samir M. El-Moghazy, Nahed M. Eid, Sahar M. Abou-Seri and Shaimaa M. Abdel-Rahman* Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University 1- Introduction and Aim Table 1 shows the percentage growth in each cell line Compounds incorporating heterocyclic ring systems continue to attract considerable interest due to the wide range of biological activities they posses. Five membered heterocycles like isoxazoline and pyrazoline are well acknowledged to possess a wide range of anticancer activities e.g. 5-(4-substituted phenyl)-3-(3,4,5-trimethoxyphenyl)-4,5-dihydro-1H-pyrazole I which are potent antitumor agents act via inhibition of tubulin polymerization.1,2 In the present study new series of isoxazoline 4a-b, pyrazoline 5a-b and 7a-f derivatives have been designed via structural modification of the lead compound I (Figure 1). They are synthesized via Claisen-Schmidt condensation followed by cyclizations with hydroxylamine HCl and hydrazine hydrate under the appropriate conditions. 2- Chemistry 4- Conclusion Several isoxazoline and pyrazoline derivatives were synthesized. Some of the new target compounds were subjected to antitumor screening against different cell lines in NCI, Maryland, U.S.A. The results showed that compound 4a displayed the highest antitumor activity against almost all cell lines while compound 7c displayed a potential antitumor activity against leukemia (SR) and colon (HT-29) cell lines. 5- References 3- Biological Evaluation Cenzo, C., Valentina, O., Loredana, V., Massimo, C. and Claudio, P.; Bioorg. Med. Chem. 2010, 18, 6238-6248. Julia, K., Renee, P., Daniele, C., Alain, C., Claude, M. and Jean-Claude, F.; Bioorg. Med. Chem. 2006, 14, 4067-4077. Screening of antitumor activity of some selected compounds against a panel of 60 cell lines in a dose of 10 uM was performed in NCI (Table 1).

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