51334-86-2Relevant articles and documents
Synthesis and in vitro anti-proliferative activity of some novel isatins conjugated with quinazoline/phthalazine hydrazines against triple-negative breast cancer MDA-MB-231 cells as apoptosis-inducing agents
Eldehna, Wagdy M.,Almahli, Hadia,Al-Ansary, Ghada H.,Ghabbour, Hazem A.,Aly, Mohamed H.,Ismael, Omnia E.,Al-Dhfyan, Abdullah,Abdel-Aziz, Hatem A.
, p. 600 - 613 (2017/11/10)
Treatment of patients with triple-negative breast cancer (TNBC) is challenging due to the absence of well- defined molecular targets and the heterogeneity of such disease. In our endeavor to develop potent isatin-based anti-proliferative agents, we utiliz
Discovery of N -(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines
Geuns-Meyer, Stephanie,Cee, Victor J.,Deak, Holly L.,Du, Bingfan,Hodous, Brian L.,Nguyen, Hanh Nho,Olivieri, Philip R.,Schenkel, Laurie B.,Vaida, Karina R.,Andrews, Paul,Bak, Annette,Be, Xuhai,Beltran, Pedro J.,Bush, Tammy L.,Chaves, Mary K.,Chung, Grace,Dai, Yang,Eden, Patrick,Hanestad, Kelly,Huang, Liyue,Lin, Min-Hwa Jasmine,Tang, Jin,Ziegler, Beth,Radinsky, Robert,Kendall, Richard,Patel, Vinod F.,Payton, Marc
, p. 5189 - 5207 (2015/08/03)
Efforts to improve upon the physical properties and metabolic stability of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compromised by increased polarity. Despite its high in vitro metabolic intrinsic cleara
Synthesis of 4-Substituted Phthalazin-1(2H)-ones from 2-Acylbenzoic Acids: Controlling Hydrazine in a Pharmaceutical Intermediate through PAT-Guided Process Development
Mennen, Steven M.,Mak-Jurkauskas, Melody L.,Bio, Matthew M.,Hollis, L. Steven,Nadeau, Kelly A.,Clausen, Andrew M.,Hansen, Karl B.
, p. 884 - 891 (2015/07/27)
A simple one-pot, two-step process for the conversion of 2-acylbenzoic acids to phthalazin-1(2H)-ones was developed. A robust process was required that delivered the final isolated solid with consistently low levels of residual hydrazine, for further processing to the final drug substance. An in situ formed intermediate was critical to control reactivity and allowed for the controlled crystallization that prevented entrainment of hydrazine. Leveraging Process Analytical Technology (PAT), we investigated the reaction profile with in situ IR and Power Compensation Calorimetry (PCC) to aid development prior to a successful scale-up.