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Scientists Synthesize New Drug Against Chemotherapy-resistant Cancer

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A team of Russian scientists led by Prof. Alexander Kiselyov from MIPT has synthesized an antitumor compound that can be used against chemotherapy-resistant cancers. The findings were published in the European Journal of Medicinal Chemistry.

Aminoisothiazole synthesis.webp

The scientists synthesized a new series of compounds called Aminoisothiazole and evaluated their anticancer effects using sea urchin embryos and human cancer cells. One of the molecules was shown to be potent and selectable.

Among the 37 compounds synthesized, 12 have different potencies to reduce the proliferation rate of cancer cells or completely prevent their division, resulting in the death of cancer cells. The action of these antineoplastic compounds is attributed to their ability to destroy microtubules involved in cell division (mitosis). Microtubules are made of a protein called tubulin, which can be targeted by anticancer agents, causing degradation of the microtubule structure.

The efficacy of synthetic compounds targeting microtubules was further evaluated using sea urchin embryos and a panel of human cancer cells from breast, melanoma, ovarian, and lung tumors. The sea urchin embryo has proven to be a good model for studying specific tubulin binders. They cause the embryo to spin rapidly instead of moving usually. This effect can be easily observed using light microscopy, allowing scientists to evaluate the anticancer potential of compounds in a short period.

In addition, the team found that sea urchin embryos were more sensitive to the drug than cancer cells. The difference between the duration of the mitotic cycle of sea urchin embryos and cancer cells (40 min vs. 24 h) may result in different effects of small molecules on tubulin dynamics and thus explain this phenomenon. A molecule characterized by 3-thiophene- and p-methoxyphenyl substituents were identified as the most potent anticancer agent under study. According to the researchers, this combination of functional groups, as well as the unique properties of the molecule, determines its activity. Specifically, the new drug exhibits anti-tubulin properties, as it blocks cell division by affecting microtubules, destroying chemoresistant cells of ovarian cancer.

The scientists plan to study microtubule degradation in more detail using crystallographic data and structural modeling techniques to identify sites where active compounds bind tubulin. In their earlier study, the researchers used substances isolated from dill and parsley seeds to synthesize another anticancer compound, glaziovianin A, and its structural analogs.

Medicilon is one of China's top drug R&D outsourcing service companies (CRO). It established the first Chinese compound synthesis, compound activity screening, structural biology, pharmacodynamics evaluation, and pharmacokinetics evaluation in Shanghai. A comprehensive technical service platform that meets international standards and is integrated with toxicological evaluation, and has been recognized by international drug management departments. Medicilon is one of the earliest Chinese local CRO companies to achieve internationalization. The animal experiment facilities have obtained the International Laboratory Animal Assessment and Accreditation (AAALAC) and the China Food and Drug Administration GLP certificate. We have reached the US Food and Drug Administration GLP standard. Medicilon will help customers achieve their goals faster with efficient and cost-effective one-stop professional services.

Medicilon can undertake the synthesis of special reagents, intermediates and molecular fragments, preparation of standard products, synthesis design and preparation of impurities or metabolites, synthesis of stable isotope internal standards and synthesis of tritiated compounds.

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