A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives was prepared using a one-pot three-component synthesis from 5-amino-1-phenyl-1H-1,2,4-triazoles, aromatic aldehydes and ethyl acetoacetate. The compound structures were confirmed by IR, ¹H-NMR, ¹³C-NMR, HRMS and X-ray analyses. The biological activity of these compounds as antitumor agents was evaluated. Their antitumor activities against cancer cell lines (MDA-MB-231 and MCF-7) were tested by the MTT in vitro method. Among them, compounds 4c and 4j displayed the best antitumor activity with IC₅₀ values of 17.83 μM and 19.73 μM against MDA-MB-231 and MCF-7 cell lines, respectively, compared to the Cisplatin reference.

Ten new differently substituted 3-benzyl-5-aryl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidin-4,6,11-triones 3 were synthesized by a simple and cost-efficient procedure in a one-pot, three-component reaction from readily available ethyl 2-amino-4-aryl-5,10-dioxo-5,10-dihydro-4H-benzo[g]chromene-3-carboxylates, benzylamine and triethyl orthoformate under solvent- and catalyst-free conditions. All the new compounds were screened for their antiproliferative activity against two colorectal-cancer-cell lines. The results showed that the compounds 3-benzyl-5-phenyl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11-trione (3a) and 3-benzyl-5-(3-hydroxyphenyl)-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11-trione (3g) exhibited the most potent balanced inhibitory activity against human LoVo and HCT-116 cancer cells.

5-fluorouracil (5-FU) is the standard of care therapy for colorectal cancer. However, complex 5-FU resistance mechanisms limit the success of this approach. Prodigiosin (PG), a secondary metabolite from various bacteria, exerts different biological activities including cancer-preventive and anticancer effects. However, studies on the anticancer effects and underlying mechanisms of PG in human colorectal and lung cancer are still limited. The present study is conducted to investigate the anticancer properties and/or adjuvant chemotherapy of PG in human colorectal and lung cancer. Cell lines HCT116, LoVo and A549 were treated with different concentrations of PG. The antiproliferative effects of PG were measured, and the apoptosis and cell cycle dynamics were assessed by flow cytometry. Our results showed that PG effectively inhibited cell proliferation and induced apoptosis. In combinatory treatment, based on PG and 5-FU, we observed a clear improvement in tumor cell proliferation inhibition. In fact, the percentage of cells in the G0/G1 phase was higher and the percentage of cells in the S phase was lower compared to treated cells separately by PG and 5-FU in all the used cell lines. Our docking studies supported targeting Akt1 by PG which could explain its proapoptotic effect separately or in combination with 5-Fu. PG obviously inhibited the tumor growth and enhanced the 5-FU therapeutic efficacy in HCT116, LoVo and A549 cells. Taken together, our findings highlight that PG effectively inhibited the growth of tumor and enhanced the sensitivity to thermotherapy, indicating PG is an inhibitor of Akt1.

Modern agricultural practices expose humans and the environment to numerous chemical pesticides. Increasing evidence suggests that commercial pesticide formulations may exhibit toxicological properties that differ from those of their active ingredients alone due to the presence of co‐formulants and additives. This study evaluated the cytotoxic and oxidative effects of commonly used commercial pesticide formulations in Tunisia on human hepatic (HepG2) and renal (HEK‐293) cell lines. The tested formulations contained deltamethrin, permethrin, abamectin, imidacloprid, mancozeb, sulfur, alpha‐chloralose, 2,4‐D‐2‐ethylhexyl ester, florasulam, cloquintocet‐mexyl, clodinafop‐propargyl, and pinoxaden. Cell viability was assessed using the MTT assay (3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide), and membrane damage was evaluated using the lactate dehydrogenase (LDH) assay. The half maximal inhibitory concentration (IC₅₀) values were determined for each formulation. Moncozeb exhibited the highest cytotoxicity in both cell lines, whereas sulfur and alpha‐chloralose showed the lowest toxicity. Intracellular reactive oxygen species (ROS) measurements revealed significant oxidative stress following exposure to several formulations, which was associated with reduced cell viability and increased LDH release. Microscopic examination further demonstrated nuclear alterations consistent with apoptosis and necrosis in exposed cells. These findings highlight the importance of evaluating complete commercial pesticide formulations, rather than active ingredients alone, when assessing potential cytotoxic and oxidative effects. The results support the inclusion of formulation‐based testing in toxicological risk assessment to better characterize potential human health hazards associated with pesticide exposure.