Boronic Acid-Containing 3H- pyrazolo[4,3-f]quinoline Compounds as Dual CLK/ROCK Inhibitors with Anticancer Properties
Neetu Dayal, Riddhi Chaudhuri, Kofi Simpa Yeboah, Nickolas R Brauer, Herman O Sintim, Luigi Panza, Daniela Imperio · 2024
Read Boronic Acid-Containing 3H- pyrazolo[4,3-f]quinoline Compounds as Dual CLK/ROCK Inhibitors with Anticancer Properties by Neetu Dayal, Riddhi Chaudhuri, Kofi Simpa Yeboah, Nickolas R Brauer, Herman O Sintim, Luigi Panza, Daniela Imperio (2024) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-11677846.txt.
Description
Neetu Dayal and co-authors built boron-bearing compounds that block two cancer-linked enzymes at once, in a study published in 2024. The enzymes, called CLK and ROCK, drive cell growth and cell movement, and each is a known drug target. Drugs that hit two targets can work harder and resist escape routes that tumors evolve. The team cooked up a library of compounds through a multi-part reaction.
Screening flagged two lead compounds that blocked the main CLK forms and ROCK2 strongly at low doses. A small chemical tweak, adding one methyl group, sharpened the second lead's selectivity. Both leads slowed kidney cancer and leukemia cells in dishes. They damaged DNA, froze the cell cycle in kidney cancer cells, and shut down a growth pathway. The authors present the pair as promising starts for boron-based cancer drugs.
Catalog record
| CREATOR | Neetu Dayal, Riddhi Chaudhuri, Kofi Simpa Yeboah, Nickolas R Brauer, Herman O Sintim, Luigi Panza, Daniela Imperio |
|---|---|
| YEAR | 2024 |
| COLLECTION | PAPERS |
| FORMAT | TXT |
| FILE SIZE | 43 KB |
| VERSION | 1.0 |
| LICENSE | CC BY 4.0 |
| RIGHTS | CC BY |
| SOURCE | Europe PMC |