5-Hydroxy-2, 3-indole Derivatives for Therapeutic Use in Treatment of Cancers and Other Diseases and Disorders Involving Excess Cell Proliferation

Life Sciences : Therapeutics

Available for licensing


  • Kimberly Kline, Ph.D. , Human Ecology
  • Marla Menchaca, M.S. , Human Ecology
  • Bob Sanders, Ph.D. , School of Biological Sciences
  • John Gilbert, Ph.D. , Chemistry and Biochemistry

Background/unmet need

The control of cell proliferation is a complex process that involves multiple interacting components. Whether a cell grows or not depends on the balance of the expression of negatively-acting and positively-acting growth regulatory genes. Negatively-acting
growth regulatory genes are those that, when expressed in or provided to a cell, lead to suppression of cell growth. Positively-acting growth regulatory genes are those which, when expressed in or provided to a cell, stimulate its proliferation.

The novel compounds and methods of present invention may be used to treat both neoplastic diseases and non-neoplastic diseases. Representative examples of neoplastic diseases are ovarian cancer, bladder cancer, lung cancer, cervical cancer, breast cancer, prostate cancer, gliomas, fibrosarcomas, retinoblastomas, melanomas, soft tissue sarcomas, ostersarcomas, colon cancer, carcinoma of the kidney, and pancreatic cancer. Representative examples of non-neoplastic diseases are psoriasis, benign proliferative skin diseases, ichthyosis, papilloma, basal cell carcinoma, squamous cell carcinoma, restinosis, scleroderma, and hemangioma.

Invention Description

University of Texas at Austin researchers have developed compounds that inhibit the division of the cells so that the tumor will stop growing (and thereby not spread to other parts of the body or systems), as well as a method to synthesize them. The 5-hydroxyy-2,3-indol derivatives were shown at various concentrations to inhibit the proliferation of human breast cancer cells and human promyelocytic leukemia cells. Six of the 18 novel compounds of the present invention are strong inhibitors of cell growth. These compounds can be delivered by a variety of methods.


  • Ocular applications through eye irrigating solution or topical optical preparation
  • Cytoprotective, anti-mitogenic, angiostatic, anti-inflammatory, anti-atherosclerotic and anti-atherogenic activities
  • Multiple pharmacological methods of delivering the drug to the affected site

Market potential/applications

There is a wide variety of pathological cell proliferative conditions for which novel methods are needed to provide therapeutic benefits. These pathological conditions may occur in almost all cell types capable of abnormal cell proliferation.

Inhibition of cell proliferation and neovascularization supports applications following intraocular lens (IOL) implantation, inhibition of cataract formation and heterodegenerative diseases, treatment for retinopathies, macular degeneration, photochemical injury, light damage injury (especially during ocular surgery).

This invention is aptly suited for the in vitro breast cancer and leukemia research market—specifically, those companies focused on inhibiting the proliferation of cell growth.

Melanoma, the most virulent of skin cancers, is a highly metastatic disease affecting both sexes and is almost uniformly fatal within five years of diagnosis. Surgical removal of localized malignancies has proven effective only when the disease has not spread beyond the primary lesion. Once the disease has spread, the surgical procedures must be supplemented with other more general procedures to eradicate the diseased or malignant cells.

Development Stage

Proof of concept

IP Status

  • 3 foreign patents application filed