Novel Thiazole Derivatives Containing Imidazole and Furan Scaffold: Design, Synthesis, Molecular Docking, Antibacterial, and Antioxidant Evaluation.

Carbothioamides , were generated in high yield by reacting furan imidazolyl ketone with -arylthiosemicarbazide in EtOH with a catalytic amount of conc. HCl. The reaction of carbothioamides , with hydrazonyl chlorides - in EtOH with triethylamine at reflux produced 1,3-thiazole derivatives -.

Discovery of New Uracil and Thiouracil Derivatives as Potential HDAC Inhibitors.

: Histone deacetylase inhibitors (HDACIs) are a relatively new class of potential drugs for treating cancer. : Discovery of new anticancer agents targeting HDAC. : New uracil and thiouracil derivatives panels were designed and synthesized as HDAC inhibitors.

New thiouracil derivatives as histone deacetylase inhibitors and apoptosis inducers: design, synthesis and anticancer evaluation.

Histone deacetylase (HDAC) inhibitors have good contributions in cancer management. To introduce new active HDAC inhibitors. Design and synthesis of 16 thiouracil derivatives with deep biological and computational investigation.

Novel pyrimidine Schiff bases and their selenium-containing nanoparticles as dual inhibitors of CDK1 and tubulin polymerase: design, synthesis, anti-proliferative evaluation, and molecular modelling.

Nanotechnology-based strategies can overcome the limitations of conventional cancer therapies. Hence, novel series of pyrimidine Schiff bases () were employed in the synthesis of selenium nanoparticle forms (). All selenium nano-sized forms exerted greater inhibitions than normal-sized compounds, far exceeding 5-fluorouracil activity.

Design, Synthesis, and Anti-Proliferative Action of Purine/Pteridine-Based Derivatives as Dual Inhibitors of EGFR and BRAF.

The investigation of novel EGFR and BRAF dual inhibitors is intended to serve as targeted cancer treatment. Two sets of purine/pteridine-based derivatives were designed and synthesized as EGFR/BRAF dual inhibitors. The majority of the compounds exhibited promising antiproliferative activity on the cancer cell lines tested.

Synthesis and study of pyrimidine-phthalimide hybrids as VEGFR2 inhibitors with antiproliferative activity.

Thalidomide, a once notorious sedative, is now clinically used as an antitumor agent. We aimed to use it as a lead compound for designing pyrimidine-phthalimide hybrids. Nucleophilic substitution reaction of thalidomide analog with primary and/or secondary aliphatic amines afforded pyrimidine-phthalimide hybrids , and .

Design, synthesis and antitumor activity of novel pyran-functionalized uracil derivatives: docking studies.

Synthesis of novel pyran-based uracils that may have potent antitumor activity against hepatocellular carcinoma HepG2 and ovarian cancer SKOV3 cell lines. Novel pyran-based uracils were synthesized and their anticancer activity was assessed using methyl thiazolyl tetrazolium and wound-healing assays to detect their cytotoxicity and their antiproliferative and antimigratory activities. Compounds , , , , , , , and significantly inhibited cell proliferation of the HepG2 cell line.

Synthesis, In Silico Prediction and In Vitro Evaluation of Antimicrobial Activity, DFT Calculation and Theoretical Investigation of Novel Xanthines and Uracil Containing Imidazolone Derivatives.

Novel xanthine and imidazolone derivatives were synthesized based on oxazolone derivatives as a key intermediate. The corresponding xanthine and imidazolone derivatives were obtained via reaction of oxazolone derivative with 5,6-diaminouracils under various conditions. Xanthine compounds were obtained by cyclocondensation of 5,6-diaminouracils with different oxazolones in glacial acetic acid.

Synthesis, In Silico Prediction and In Vitro Evaluation of Antitumor Activities of Novel Pyrido[2,3-]pyrimidine, Xanthine and Lumazine Derivatives.

Ethyl 5-arylpyridopyrimidine-6-carboxylates - were prepared as a one pot three component reaction via the condensation of different aromatic aldehydes and ethyl acetoacetate with 6-amino-1-benzyluracil under reflux condition in ethanol. Additionally, condensation of ethyl 2-(2-hydroxybenzylidene) acetoacetate with 6-amino-1-benzyluracil in DMF afforded 6-acetylpyridopyrimidine-7-one ; a facile, operationally, simple and efficient one-pot synthesis of 8-arylxanthines - is reported by refluxing 5,6-diaminouracil with aromatic aldehydes in DMF. Moreover, 6-aryllumazines - was obtained via the reaction of 5,6-diaminouracil with the appropriate aromatic aldehydes in triethyl orthoformate under reflux condition.

A Novel Synthesis of Fused Uracils: Indenopyrimidopyridazines, Pyrimidopyridazines, and Pyrazolopyrimidines for Antimicrobial and Antitumor Evalution.

A variety of different compounds of fused uracils were prepared simply by the heating of 6-hydrazinyl-1-methyl-, 6-hydrazinyl-1-propyl-, or 6-hydrazinyl-1,3-dipropyluracil under reflux with ninhydrin, isatin, benzylidene malononitrile, benzylylidene ethyl cyanoacetate, benzil, and phenacyl bromide derivatives. The newly synthesized compounds were completely screened for antimicrobial and antitumor activity.