Challenging breast cancer through novel sulfonamide-pyridine hybrids: design, synthesis, carbonic anhydrase IX inhibition and induction of apoptosis.

Among the important key modulators of the tumor microenvironment and hypoxia is a family of enzymes named carbonic anhydrases. Herein, 11 novel sulfonamide-pyridine hybrids () were designed, synthesized and biologically evaluated for their potential use in targeting breast cancer. The para chloro derivative reported the highest cytotoxic activity against the three breast cancer cell lines used.

Synthesis of novel benzothiophene derivatives as protectors against cranial irradiation-induced neuroinflammation.

Cranial irradiation results in many deleterious effects to normal tissues, including neuroinflammation. There is a need to explore radioprotective agents that could be safely used to ameliorate these effects. Nine novel benzothiophene derivatives bearing pyrimidinone, pyrazolidinone, triazole and other active moieties were synthesized and evaluated as antioxidants in an screening experiment.

Green synthesis of novel antifungal 1,2,4-triazoles effective against γ-irradiated Candida parapsilosis.

This study reports the green synthesis of 11 novel 3-substituted-4-amino-5-mercapto-1,2,4-triazole derivatives using water as a readily available nontoxic solvent. Evaluation of their antimicrobial potential against several clinical pathogenic microorganisms was carried out. The newly synthesized cysteine derivative 6 showed promising antifungal activity against both γ-irradiated and nonirradiated Candida parapsilosis 216, with the lowest MIC (minimum inhibitory concentration) value of 3.

Anti-inflammatory, analgesic and COX-2 inhibitory activity of novel thiadiazoles in irradiated rats.

In this work, novel series of pyran, thiophene and thienopyrimidine derivatives based on 2-acetamide-thiadiazole scaffold were designed and synthesized for evaluation as selective COX-2 inhibitors in-vitro and investigated in-vivo as anti-inflammatory and analgesic agents against carrageenan-induced rat paw oedema model in irradiated rats, since its well-known that ionizing radiation plays an important role in exaggerating the inflammatory responses and in enhancing the release of inflammatory mediators in experimental animals. Toxicological studies were carried out to evaluate the ulcerogenic activity, acute toxicity and kidney and liver functions for the most potent compounds. In order to understand the binding mode of the synthesized compounds into the active site of COX-2, docking study was performed.

Anticancer and radio-sensitizing evaluation of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety.

Recently, it has been reported that compounds bearing a sulfonamide moiety posses many types of biological activities, including anticancer activity. There are a variety of mechanisms for their anticancer activity, and the most prominent mechanism is the inhibition of carbonic anhydrase (CA) isozymes. The present work reports the synthesis of some new thiazolo[4,5-b]pyrane, thiazolo[4,5-b]pyrano[2,3-d]pyrimidine derivatives bearing a sulfonamide moiety.