New Chalcone Incorporated Structurally Modified Pyridine-Pyrimidine Derivatives as Anticancer Agents: Their Design, Synthesis, and in-vitro Evaluation.

Chalcone-incorporated pyridine-pyrimidines i.e. derivatives of (5-(6-(pyrimidin-5-yl)pyridin-3-yl)thiophen-2-yl)prop-2-en-1-one were synthesized and their structures were confirmed by analytical techniques.

Synthesis, biological evaluation and docking studies of 1,2,4-oxadiazole linked 5-fluorouracil derivatives as anticancer agents.

Background: 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors.

Synthesis of 2-cyclopropyl-3-(5-aryl-1H-pyrazol-3-yl)-1,8-naphthyridine.

Background: 1,8-Naphthyridine derivatives have attracted considerable attention because the 1,8-naphthyridine skeleton is present in many compounds that have been isolated from natural substances, with various biological activities.

Findings: N,N-dimethoxy-N-methyl-1,8-naphthyridine-3-carboxamide (1) on reaction with Grignard reagent forms 2-methoxy-1,8-naphthyridine-3-carbaldehyde (2). Compound 2 on reaction with different aromatic aldehydes provided 1-(2-cyclopropyl-1,8-naphthyridin-3-yl)-3-arylprop-2-en-1-ones (3a-e) and these compounds on cyclisation with hydrazine hydrate 99% yielded 2-cyclopropyl-3-(5-aryl-1H-pyrazol-3-yl)-1,8-naphthyridines (4-a-e).

Synthesis and biological evaluation of benzimidazole-linked 1,2,3-triazole congeners as agents.

Background: Benzimidazoles and triazoles are useful structures for research and development of new pharmaceutical molecules and have received much attention in the last decade because of their highly potent medicinal activities.

Findings: A simple and efficient synthesis of triazole was carried out by treatment of 2-(4-azidophenyl)-1H-benzo[d]imidazole (6) with different types of terminal alkynes in t-BuOH/H2O, sodium ascorbate, and Zn(OTf)2, screened for cytotoxicity assay and achieved good results. A series of new benzimidazole-linked 1,2,3-triazole (8a-i) congeners were synthesized through cyclization of terminal alkynes and azide.

Synthesis and antibacterial activity of novel 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide derivatives.

Background: The intensely increasing multi-drug resistant microbial infections have encouraged the search for new antimicrobial agents. Hydrazone derivatives are known to exhibit a wide variety of biological activities including anti-microbial. In heterocyclic moiety, imidazo[1,2-a]pyrimidines are the subject of immense interest for their antimicrobial activity and also for their analgesic, antipyretic and anti-inflammatory properties.