Browsing by Author "Mohareb, Rafat M."

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Heterocyclic ring extension of androstenedione: Synthesis and cytotoxicity of fused pyran, pyrimidine and thiazole derivatives
(ELSEVIER, 2014) Mohareb, Rafat M.; Abbas, Nermeen S.; Abdelaziz, Mahmoud A.
The reaction of androstenedione with either malononitrile or ethyl cyanoacetate and aromatic aldehydes 2a-c gave the pyran derivatives 4a-f, respectively. On the other hand, the reaction of androstenedione with thiourea and the aromatic aldehydes 2a-c gave the pyrimidine derivatives 6a-c, respectively. Compound 6b reacted with 2-bromo-1-arylethanone derivatives 7a-d to give the indeno[2,1-e]thiazole derivatives 8a-d. Some of the produced compounds were used for further heterocyclization reactions. The cytotoxicity of the newly obtained products was evaluated against some cancer cell lines and a normal cell line. (C) 2014 Elsevier Inc. All rights reserved.
New approaches for the synthesis of pyrazole, thiophene, thieno[2,3-b]pyridine, and thiazole derivatives together with their anti-tumor evaluations
(SPRINGER BIRKHAUSER, 2014) Mohareb, Rafat M.; Abdallah, Amira E. M.; Abdelaziz, Mahmoud A.
The reaction of cyanoacetylhydrazine (1) with acetylchloride (2) gave the N-acyl derivative 3. The latter underwent ready cyclization in sodium ethoxide to give the pyrazole derivative 4 which was the key compound for the synthesis of thiophene, thieno[2,3-b]pyridine, and thiazole derivatives. The anti-tumor evaluations of the newly synthesized products against the three human tumor cell lines, namely, breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460), and CNS cancer (SF-268), were studied. Some of these compounds were found to exhibit much higher inhibitory effects toward the three tumor cell lines than the reference doxorubicin. Molecular modeling of the four compounds 12c, 12f, 16a, and 16d, which showed the maximum inhibitory effect, were done.
The reaction of beta-amino-alpha,gamma-dicyanocrotononitrile with acetophenone: Synthesis of pyridine, pyridazine and thiophene derivatives with antimicrobial activities
(HRVATSKO FARMACEUTSKO DRUSTOV (HFD)-CROATION PHARMACEUTICAL SOC., 2008) Mohareb, Rafat M.; El-Sharkawy, Karam A.; Sherif, Sherif M.
Condensation of beta-amino-alpha,gamma-dicyanocrotononitrile (1) with acetophenone gave 2-amino-4-phenylpenta-1,3-diene-1,1,3-tricarbonitrile (2). The latter product was used in a series of heterocyclization reactions with different reagents such as diazonium salts, hydrazines, hydroxylamines and elemental sulfur to give pyridazine, pyrazole, isoxazole and thiophene derivatives, respectively. On the other hand, it gave pyridine derivatives with aromatic aldehydes folowed by reaction with cyanomethylene reagents. The MIC values for the newly synthesized product were measured against E. coli, B. cereus, B. subtilis and C. albicans.
The utilization of 2-aminoprop-1-ene-1,1,3-tricarbonitrile as a precursor to quinoline, furan and thiophene derivatives with antitumor activities
(WALTER DE GRUYTER & CO, 2011) Mohareb, Rafat M.; Fleita, Daisy H.; Sakka, Ola K.
The condensation reaction of 2-aminoprop-1-ene-1,1,3-tricarbonitrile (1) with 2-acetyl-furan (2) afforded 2-amino-4-(furan-2-yl)penta-1,3-diene-1,1,3-tricarbonitrile (3). The latter compound underwent a series of heterocyclization reactions to give quinoline, furan, pyrazole and thiophene derivatives. The antitumor evaluation of the newly synthesized products against three cancer cell lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) were recorded. Three of the synthesized compounds, namely 4, 5d and 12 showed high inhibitory effects.