Indole compounds and their use as radiation sensitizing agents and chemotherapeutic agents

Radiotherapy is the treatment of cancer and other diseases with ionizing radiation. Radiotherapy is used in curative therapy, palliative therapy, adjuvant therapy after or before surgery, simultaneous radio-chemotherapy, etc. Radiotherapy is successful because ionizing radiation kills dividing cells and is thus slightly more toxic to fast growing cancer cells. Radiotherapy may be used to treat localized solid tumors, such as cancers of the skin, tongue, larynx, brain, breast, or uterine cervix. Agents which are used to potentiate the effectiveness of radiation therapy in destroying unwanted cells are radiation sensitizing agents. Various attempts have been made to develop a radiation sensitizer that reduces the radiation dose and adverse drug reactions without compromising the therapeutic effect of radiotherapy. The indole derived Aplysinopsin analogs have been reported as potent and selective cytotoxic agents against cancer cells. These observations prompted us to design and synthesize a series of novel indole derivatives, including substituted 5((N-Benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones & (Z)-5((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-diones and their related compounds with various substitutions on both the indolic ring and the N-benzyl group that are radiation sensitizers. These compounds produced robust radiosensitization in several cancer cell lines that include lung, pancreatic, glioblastoma, colon, and breast. The compounds suppressed tumor growth in vivo models.

Attached files:
YTR107 CCR paper.pdf
YTR BMCL paper.pdf

US 8,304,421 issued 2012-11-06   [MORE INFO]

Type of Offer: Licensing

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