A series of benzo[h]chromenes, benzo[f]chromenes, and benzo[h]chromeno[2,3-d]pyrimidines were prepared. All the newly synthesised compounds were selected by National Cancer Institute for single-dose testing against 60 cell lines. Benzo[h]chromenes 5a and 6a showed promising anti-cancer activity and selected for the five-dose testing. Compounds 5a and 6a suppressed cell growth in HL-60 by the induction of cell cycle arrest, which was confirmed using flow cytometry and Annexin V-FITC/PI assays showed at the G1/S phase by regulating the expression of CDK-2/CyclinD1, triggering cell apoptosis by activating both the extrinsic (Fas/Caspase 8) and intrinsic (Bcl-2/Caspase 3) apoptosis pathways, which were determined by the western blot. Benzo[h]chromenes 5a and 6a decreased the protein expression levels of Bcl-2, CDK-2, and CyclinD1 and increased the expression of caspase 3, caspase 8, and Fas. In silico molecular analysis of compounds 5a and 6a in CDK-2 and Bcl-2 was performed.

Since herpes simplex virus type 1 (HSV-1) infection is so widespread, several antiviral drugs have been developed to treat it, among which are uracil nucleosides. However, there are major problems with the current medications such as severe side-effects and drug resistance. Here we present some newly synthesized cyclic and acyclic uracil nucleosides that showed very promising activity against HSV-1 compared to acyclovir.

The leading cause of death worldwide is reportedly cancer. This deadly, multigenetic condition is characterized by unchecked cell proliferation and differentiation. A family of protein kinases known as tyrosine kinases is essential for cancer cell survival and metastasis. The fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR), and epidermal growth factor receptor (EGFR) are members of this family of kinases. As a result of medication resistance and systemic toxicity brought on by current cancer treatments, the development of novel anticancer agents is urgently necessary. One of the main goals of creating new, strong anticancer drugs is to prevent angiogenesis by reducing VEGFR-2 activity. The effectiveness of novel synthesised pyrrolotriazolopyrimidine derivatives 6a,b against sixty human cancer cell lines from nine different cancer types was evaluated. The results were analyzed, and molecular docking was used to simulate the inhibitory activity of compounds 6a and b on VEGFR-2. Spectroscopic examination supported the chemical structure of 6a,b.

Radiopharmaceutical applications in tumor imaging are widely used nowadays. Radioisotopes alone cannot reach the tumor easily, so it can be linked to a carrier to deliver the radioisotope to the tumor site. Theses carriers could be peptides, antibodies or small chemical agents. In our study, gallic acid derivative (4) and vanillin derivative (6) were used as two targeting chemical agents to be linked with 99mTc to prepare 99mTc-4 and 99mTc-6, then these two radiopharmaceutical were injected into mice and T/NT results were recorded for both of 99mTc-4 and 99mTc - 6 after 15 min, 30 min, 60 min and 180 min. T/NT for 99mTc-4 and 99mTc-6 at 60 min 1.74 and 4.32 respectively compared with the reference value for T/NT 1.5. These can conclude that 99mTc-4 and 99mTc-6 have a powerful targeting toward tumor, so that these two chemical agents 4 and 6 are promising to be applied into radiopharmaceutical applications.