Magdi E. A. Zaki

By Ayesha Rafiq, Sana Aslam, Matloob Ahmad, Muhammad Jawwad Saif, Sami A. Al-Hussain and Magdi E.A. Zaki

Heterocyclic ring systems are gaining attention due to their pivotal role in drug design and medicinal chemistry. Quinazolines are nitrogen-containing heterocyclic pharmacophoric units found in abundance in natural and pharmaceutical products. Imidazoquinazolines and benzimidazoquinazolines are fused tricyclic and tetracyclic heterocyclic moieties, respectively. Different isomeric forms of imidazoquinazolines and benzimidazoquinazolines exhibited a plethora of biological applications such as antitumor, antimicrobial, antioxidant, anti-inflammatory, antitubercular, anticancer, antihypertensive, anticonvulsant, antiviral, antimalarial, antiapoptotic, anti-proliferative activities, etc. This chapter addressed the recent synthetic strategies for medicinally privileged scaffolds; imidazoquinazolines and benzimidazoquinazolines. The synthetic routes of various isomeric forms of above-mentioned heterocycles have also been discussed.

Part of the book: Recent Advances on Quinazoline

By Tooba Jabeen, Sana Aslam, Matloob Ahmad, Atta ul Haq, Sami A. Al-Hussain and Magdi E.A. Zaki

Triazoloquinazoline is a fused heterocyclic nucleus, formed by the fusion of two fundamental heterocyclic moieties; triazole and quinazoline. This class of compound is known for its potential as a therapeutic agent and is endowed with several pharmacological applications. Triazoloquinazoline and its derivatives have shown a variety of biological applications such as anticancer, anti-inflammatory, antimicrobial, antiviral, antihypertensive, anticonvulsant, antidiabetic, antioxidant, adenosine receptor antagonist, and significant cytotoxic activities. Hence, this privileged scaffold could act as an important candidate in the field of drug development. Many synthetic protocols have been developed to efficiently synthesize this fused heterocycle and its derivatives. Triazole and quinazoline rings fused at different positions which occurs in various isomeric forms such as, 1,2,4-triazolo[1,5-c]quinazoline, 1,2,4-triazolo[1,5-a]quinazoline, 1,2,4-triazolo[4,3-c]quinazoline, 1,2,4-triazolo[4,3-a]quinazoline, etc. This book chapter covers the synthesis of various isomeric forms of triazoloquinazoline as well as their biological activities.

Part of the book: Recent Advances on Quinazoline

By Sadia Rani, Samina Aslam, Ali Irfan, Emilio Mateev, Sami A. Al-Hussain and Magdi E.A. Zaki

The profound pharmacological attributes of macrocyclic compounds have spurred their transformation into pharmaceutical drugs. Within conformationally pre-organized ring structures, the macrocycle’s intricate functions and stereochemical complexity contribute to a heightened affinity and selectivity for protein targets. Simultaneously, they maintain sufficient bioavailability to penetrate intracellular locations. As a result, the construction of macrocycles emerges as an optimal strategy for addressing the challenge of “undruggable” targets like cancer. Cancer stands as the second most prevalent and formidable threat to human life, prompting researchers to channel their efforts toward the extraction and synthesis of effective therapeutic drugs designed on macrocyles to combat various types of cancer cells. Many macrocyclic drugs have been licensed by the Food and Drug Administration (FDA) for the treatment of cancer patients. Nonetheless, the significance of these compounds in the production of cancer therapeutics is still undervalued. According to recent research, macrocyclic compounds can be a useful tactic in the fight against drug resistance in the treatment of cancer. This chapter aims to present bits of evidence about the uses of macrocyclic compounds as potential cancer treatments. By providing more innovative approaches to aid cancer patients and society as a whole, this chapter will hopefully stimulate greater interest in the development of macrocyclic medicines for cancer therapy.

Part of the book: Heterocyclic Chemistry - New Perspectives [Working title]