Russian scientists from RANEPA, with support from the Russian Science Foundation, have developed a fundamentally new type of chemotherapeutic molecules—hybrid compounds that proved 1.5 times more effective than osimertinib, one of the costliest and most advanced drugs against resistant forms of cancer. According to the RSF press service, the key to success was adding just one chlorine atom to the molecular structure, which turned the substance into an “ideal key” for the cancer cell receptor. Senior researcher at RANEPA, Olga Mikolaichuk, explained that according to the rules of medicinal chemistry, a molecule must fit the body’s receptor like a key in a lock, and thanks to chlorine, this key fit perfectly, halting tumor cell division and leading to their death.
Most modern chemotherapy drugs work by blocking the epidermal growth factor receptor (EGFR) on the surface of cancer cells, which controls their uncontrolled proliferation. However, mutations in EGFR’s structure often render these drugs ineffective. Scientists created a hybrid molecule that combines two distinct compounds, capable of targeting tumor cells through multiple pathways simultaneously. It turned out that one such molecule, consisting of two nitrogen-containing ring structures, gains potent anticancer properties when a single chlorine atom is introduced.
Thanks to this, the new compound can bind to EGFR not only at the active site but also at its peripheral regions, which are unaffected by mutations. Even without chlorine, the molecule effectively destroys lung, liver, colorectal, and breast cancer cells, comparably to osimertinib. Adding chlorine boosts its activity by 1.5 times, which could ultimately make therapy for resistant tumors not only more powerful but also more affordable by reducing treatment costs. This discovery, according to researchers, opens new horizons for creating cheap and highly effective drugs against resistant forms of cancer, which remain among the most difficult to treat today.
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