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Arch Pharm (Weinheim) 2021 Mar 23;354(3):e2000237. Epub 2020 Nov 23.

Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.

A new series of 1,2,4-triazolo[4,3-c]quinazoline derivatives was designed and synthesized as Topo II inhibitors and DNA intercalators. The cytotoxic effect of the new members was evaluated in vitro against a group of cancer cell lines including HCT-116, HepG-2, and MCF-7. Compounds 14 , 14 , 14 , 14 , 15 , 18 , 18 , and 19 exhibited the highest activities with IC values ranging from 5. Read More

Anticancer Agents Med Chem 2020 Nov 10. Epub 2020 Nov 10.

Training Sector, Ministry of Military Production, Alsalam City, Cairo, A. R.. Egypt.

Background: Recently multi-component reactions producing pyran and pyridine derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Through the market it was found that many pharmacological drugs containing the pyran and pyridine nucleus were known.

Objective: We are aiming in this work to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. Read More

Acta Chim Slov 2017 Dec;64(4):988-1004

A microwave-assisted, environmentally benign green protocol for the synthesis of functionalized (Z)-3-(2-oxo-2-phenylethylidene)-3, 4-dihydro-2H-benzo[b][1,4]oxazin-2-ones (11a-n) in excellent yields (upto 97%) and (Z)-3-(2-oxo-2-phenylethylidene)-3,4-dihydroquinoxalin-2(1H)-ones (14a-h) (upto 96% yield) are reported. The practical applicability of developed methodology were also confirmed by the gram scale synthesis of 11a, 14c and 14e; synthesis of anticancer alkaloid Cephalandole A 16 (89% yield). All the synthesized compounds 11a-n, 14a-h and 16 were assessed for their in vitro antioxidant activities in DPPH radical scavenging and FRAP assay. Read More

Tetrahedron 2017 Jul 15;73(30):4493-4500. Epub 2017 Jun 15.

Department of Chemistry, Marquette University, P. O. Box 1881, Milwaukee, WI 53201-1881 USA.

The reaction of tricarbonyl and (dicarbonyl)triphenylphosphine (1-methoxycarbonyl-pentadientyl)iron(1+) cations and with methyl lithium, NaBHCN, or potassium phthalimide affords (pentenediyl)iron complexes and , while reaction with dimethylcuprate, gave (,-diene)iron complexes and . Oxidatively induced-reductive elimination of gave vinylcyclopropanecarboxylates . The optically active vinylcyclopropane (+)-, prepared from (1)-, undergoes olefin cross-metathesis with excess (+)- to yield (+)-, a C9-C16 synthon for the antifungal agent ambruticin. Read More

Arch Toxicol 2017 Aug 18;91(8):2827-2835. Epub 2017 May 18.

Department of Pharmacology and Toxicology and James Graham Brown Cancer Center, University of Louisville School of Medicine, Louisville, KY, 40202, USA.

Human N-acetyltransferase 2 (NAT2) catalyzes the N-acetylation of numerous aromatic amine drugs such as sulfamethazine (SMZ) and hydrazine drugs such as isoniazid (INH). NAT2 also catalyzes the N-acetylation of aromatic amine carcinogens such as 2-aminofluorene and the O- and N,O-acetylation of aromatic amine and heterocyclic amine metabolites. Genetic polymorphism in NAT2 modifies drug efficacy and toxicity as well as cancer risk. Read More