Band 31, Heft 1

Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunomodulatory enzyme associated with tumor immune evasion, making it a promising target for cancer therapy. This study aimed to identify novel holo-IDO1 inhibitors with distinct structural scaffolds. A series of theophylline derivatives containing 1,2,3-triazole groups were designed and synthesized through the condensation of theophylline acetic acid and 4-aminophenylacetylene. Among the synthesized compounds, 3c and 3e exhibited the most potent inhibitory effects in IDO1 enzymatic activity assays. Molecular docking and affinity prediction analyses provided insights into the binding affinities and mechanisms of action of the lead compounds. Our findings suggest that theophylline derivatives are promising holo-IDO1 inhibitors, warranting further development for potential therapeutic applications.

The synthesis of 1,2,3-triazoles, which are acting as promising pharmacophores with strong biological activity, is the focus of our work. Three obscure streaks of hybrid molecules with a 1,2,3-triazole nucleus have been synthesized by us. Compounds are synthesized in two steps: first, an azide is formed from its amine equivalent, next 1,2,3-triazole ring is formed utilizing azide-alkyne click chemistry. The obtained yields range from fair to good. After testing, it is discovered that the compounds 1c, 2a, 2c, 3a have good antibacterial properties and compounds 2b, 3a have promising antifungal properties. The compounds are found to be soluble in ethanol, ethyl acetate. The primary difficulty we encountered was with cyclopropane as the reaction needed to be carried out under reflux at 100°C, and its boiling point is 51°C.

A novel series of triazolothiadiazines has been successfully synthesized with high efficiency through Knoevenagel condensation, utilizing thiocarbamoyl dihydrazine as the starting material. The structures of these compounds were characterized through 1 H-NMR, 13 C-NMR, high-resolution mass spectrometry. The MTT assay was utilized to evaluate the in vitro cytotoxicity of the synthesized compounds against four human cancer cell lines including SW620, A549, Hela, and MCF-7. Among the tested compounds, (Z)-3-methyl-6-phenyl-7-(3-(trifluoromethyl)benzylidene)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine exhibited notably potent antiproliferative activity against all four human cancer cell lines. Graphical abstract

This review article summarizes the role of heterocyclic compounds as anticancer drugs used against various human cancers, including doxorubicin, cisplatin, paclitaxel, and resveratrol, which are among the most effective therapeutic agents. Chemotherapy, a treatment modality, exerts its effects on tumor cell DNA and often involves the use of low-molecular-weight medicines to selectively target and destroy cancer cells. However, systemic chemotherapy is associated with several side effects, such as nausea, vomiting, myelosuppression, and cardiotoxicity. Cancer remains one of the most prevalent and lethal diseases, characterized by uncontrolled cell division and abnormal cell growth driven by multiple genetic mutations. The etiopathogenesis of cancer is complex, but significant advancements have been made in treatment, particularly with the discovery of anticancer drugs, including cytotoxic chemotherapy, hormonal agents, and targeted therapies. Anticancer drugs are widely employed for the treatment of various cancers, such as breast, cervical, uterine, and kidney cancers. These drugs are classified into several categories, including alkylating agents, antimetabolites, antibiotics, and topoisomerase inhibitors. Among these, numerous heterocyclic compounds have shown promising anticancer properties. The goal of this review is to compile information on heterocyclic compounds used as anticancer drugs, highlighting their positive effects and therapeutic targets in cancer treatment and chemoprevention.