Quinazoline-thiohydantoin Fused Heterocycles Which Are Suitable for Treating, Ameliorating or Preventing a Proliferative Disorder

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The patent discloses a new class of chemical compounds called quinazoline-thiohydantoin fused heterocycles and their use as potential therapeutic agents for treating proliferative disorders like cancer, especially leukemia. These compounds have shown significant effectiveness against drug-resistant cancers, such as multidrug-resistant leukemia, by inhibiting cell proliferation and overcoming resistance mechanisms. The patent also provides efficient, metal-free synthesis methods for producing these novel compounds and their pharmaceutical compositions.

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• Treatment of leukemia, especially forms that are resistant to multiple drugs.
• Therapy for other proliferative disorders, including various types of cancer (e.g., breast, skin, lung, cervical cancers).
• Potential use in overcoming chemotherapy resistance in cancer treatment regimens.
• Development of combination therapies alongside existing anti-cancer drugs to enhance effectiveness against resistant tumors.
• Research tool for studying mechanisms of drug resistance and cell proliferation in cancer biology.

BenefitsContent extracted from patent full text and abstract with AI.

• Significantly higher activity against multidrug-resistant leukemia cells compared to standard drugs (e.g., doxorubicin).
• Selectively targets cancer cells with much lower toxicity to healthy human cells.
• Enables treatment options for patients who have failed existing chemotherapy due to drug resistance.
• Provides new molecular scaffolds for anti-cancer drug development, expanding options for medicinal chemistry.
• One-pot, metal-free synthetic route allows for operational simplicity and high yields, facilitating large-scale production.
• Potential to inhibit tumor growth by affecting important biological pathways (e.g., suppressing MRTF-A nuclear localization) related to drug resistance and cell proliferation.

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Patent Abstract

The present invention refers to quinazoline-thiohydantoin fused heterocycles having the formula (I). The compounds are suitable for treating, ameliorating or preventing a proliferative disorder, such as leukemia, and are useful for treating or ameliorating a multidrug resistant proliferative disorder, such as multidrug resistant leukemia.