Compounds > 3-hydroxy-quinazoline-2-4-dione

3-hydroxy-quinazoline-2-4-dione and Urinary-Bladder-Neoplasms

3-hydroxy-quinazoline-2-4-dione has been researched along with Urinary-Bladder-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for 3-hydroxy-quinazoline-2-4-dione and Urinary-Bladder-Neoplasms

Article	Year
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors. Bioorganic & medicinal chemistry letters, 2005, Jan-17, Volume: 15, Issue:2 Flap endonuclease-1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. Sensitization to DNA damaging agents is a potential method for the improvement of the therapeutic window of traditional chemotherapeutics. In this paper, we describe the identification and SAR of a series of low nanomolar FEN1 inhibitors. Over 1000-fold specificity was achieved against a related endonuclease, xeroderma pigmentosum G (XPG). Two compounds from this series significantly potentiate the action of methyl methanesulfonate (MMS) and temozolamide in a bladder cancer cell line (T24). To our knowledge, these are the most potent endonuclease inhibitors reported to date. Topics: Cell Line, Tumor; Dacarbazine; DNA Damage; Enzyme Inhibitors; Flap Endonucleases; Humans; Methyl Methanesulfonate; Structure-Activity Relationship; Temozolomide; Urea; Urinary Bladder Neoplasms; Xeroderma Pigmentosum	2005

Article

Year

The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.

Bioorganic & medicinal chemistry letters, 2005, Jan-17, Volume: 15, Issue:2

Flap endonuclease-1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. Sensitization to DNA damaging agents is a potential method for the improvement of the therapeutic window of traditional chemotherapeutics. In this paper, we describe the identification and SAR of a series of low nanomolar FEN1 inhibitors. Over 1000-fold specificity was achieved against a related endonuclease, xeroderma pigmentosum G (XPG). Two compounds from this series significantly potentiate the action of methyl methanesulfonate (MMS) and temozolamide in a bladder cancer cell line (T24). To our knowledge, these are the most potent endonuclease inhibitors reported to date.

Topics: Cell Line, Tumor; Dacarbazine; DNA Damage; Enzyme Inhibitors; Flap Endonucleases; Humans; Methyl Methanesulfonate; Structure-Activity Relationship; Temozolomide; Urea; Urinary Bladder Neoplasms; Xeroderma Pigmentosum

2005