With the participation of the ZIOC photopharmacological agents are being developed for the treatment of epidermoid carcinoma

The use of light-sensitive small molecules as inhibitors of tubulin polymerization may be one of the solutions to the problems of specificity of anticancer drugs. However, photodegradation of potential photopharmacological agents is one of the most serious limitations of this approach. For this reason, a comprehensive photochemical study of potential biologically active compounds is an important task for the development of effective anticancer drugs, the activity of which will be controlled by the action of light.

Researchers of the Laboratory of Heterocyclic Compounds of the Zelinsky Institute in cooperation with Blokhin National Medical Research Center of Oncology, for the first time synthesized quinazoline derivatives, which are stilbene analogs of combretastatin A-4, a natural compound that exhibits strong cytotoxic activity against a wide range of human cancer cell lines. The photochemical properties of the synthesized compounds were studied in detail, and their antiproliferative activity against human epidermoid carcinoma cells was investigated. The leader structure induces apoptosis of cancer cells at submicromolar concentrations. An interesting finding is that the antiproliferative activity of the resulting molecules can be controlled by changing the ratio of the E- and Z-forms. This discovery can be considered as a starting point for the study of the quinazoline analogs of combretastatin A-4 as promising innovative therapeutic agents for the treatment of epidermoid carcinoma.

Source:

A. M. Scherbakov, R. Yu. Balakhonov, D. I. Salnikova, D. V. Sorokin, A. V. Yadykov, A. I. Markosyan, V. Z. Shirinian Light-driven photoswitching of quinazoline analogues of combretastatin A-4 as an effective approach for targeting skin cancer cells Org. Biomol. Chem., 2021, 19, 7670–7677. DOI: 10.1039/d1ob01362a.