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Pyrazole-Indole Hybrids For Photodynamic Treatment
Photodynamic therapy (PDT) is a non-surgical, minimally invasive treatment which uses light-sensitive medication (photosensitizer, PS), light source and oxygen to produce cytotoxic reactive oxygen species (ROS), which in turn cause abnormal cell destruction. Nowadays, several skin conditions, such as psoriasis, acne, bacterial infections, as well as various types of cancer such as basal cell carcinoma, squamous cell carcinoma, melanoma, lung, head, mouth, nasopharyngeal, laryngeal, bladder, vaginal or cervical cancers can be treated using PDT. The trend of the cancer incidence rate is increasing at 0.6% every year. Although such diseases are increasingly detected unusually in young patients worldwide, the highest rates of cancer incidence are observed in the elderly (80-84 years and older) age groups.
The invention relates to new conjugated pyrazole-indole derivatives, which possess low dark toxicity while exhibiting photodynamic properties against cancer cell lines and bacteria under light conditions. The invention also describes a method of production of said new compounds and intermediates for preparation thereof, and use of the new compounds as medicaments.
Technology Features, Specifications and Advantages
The invention relates to new pyrazole-indole hybrids conjugated by ethene, buta-1,3-diene or ethyne linkers and containing substituents at R1, R2 and R3 positions of the general formula I.
After a pre-incubation with conjugated pyrazole-indole derivatives of the general formula I, light irradiation is applied to the treatment site. The preferred wavelength of the activating light irradiation is between 400 nm and 450 nm, preferably corresponding to the maximum absorption of the given compound of formula I. The irradiation can be performed using a non-coherent radiation such as from a diode-based source, or using a coherent radiation such as laser radiation. For surface treatments, a light source may be effective in irradiating specific target areas; for lesions within the body (inner cavities), an optical fiber apparatus or other devices may be used to irradiate target areas.
The invention further relates to a pharmaceutical composition, which comprises at least one conjugated pyrazole-indole derivative of the general formula I, and a pharmaceutically acceptable carrier.
The present invention provides a series of novel substituted pyrazole-indole conjugated derivatives that are useful for photodynamic therapy. Hence, they can be used as anticancer agents, antibacterial agents and antibiotics.
- The developed substances help to treat skin cancer or epithelial tumors
- The substances act as photosensitizing agents in photodynamic therapy.
- Non-invasive method of treatment
- Low toxicity
- Antibacterial properties
- Hybrids can be used as antimicrobial photosensitizing agents which have antimicrobial activity against at least Gram-positive bacteria.