303777-04-0Relevant articles and documents
Design, synthesis and molecular modeling of new quinazolin-4(3H)-one based VEGFR-2 kinase inhibitors for potential anticancer evaluation
Abdallah, Abdallah E.,Eissa, Sally I.,Al Ward, Maged Mohammed Saleh,Mabrouk, Reda R.,Mehany, Ahmed B.M.,El-Zahabi, Mohamed Ayman
, (2021)
Globally cancer is the second leading cause of death. So that this work is an attempt to develop new effective anti-cancer agents. In line with pharmacophoric features of VEGFR-2 kinase inhibitors, new nineteen quinazolin-4-one derivatives were designed,
Design, synthesis and biological activity evaluation of 2-mercapto-4(3H)-quinazolinone derivatives as novel inhibitors of protein tyrosine phosphatase 1B
Li, Hui,Wang, Jin-Ping,Yang, Fan,Liu, Ting,Qiu, Wen-Wei,Li, Jing-Ya,Li, Jia,Tang, Jie
experimental part, p. 1897 - 1911 (2012/09/07)
A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC50 = 1.50 μ ;g/mL), and 27 possessed the best selectivity of 3.0-fold.
