Chen Ping, Iwanowicz Edwin J, Norris Derek, Gu Henry H, Lin James, Moquin Robert V, Das Jagabandhu, Wityak John, Spergel Steven H, de Fex Henry, Pang Suhong, Pitt Sydney, Shen Ding Ren, Schieven Gary L, Barrish Joel C
Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA.
Bioorg Med Chem Lett. 2002 Nov 4;12(21):3153-6. doi: 10.1016/s0960-894x(02)00677-7.
A series of anilino(imidazoquinoxaline) analogues bearing solubilizing side chains at the 6- and 7-positions of the fused phenyl ring has been prepared and evaluated for inhibition against Lck enzyme and of T-cell proliferation. Significant improvement of the cellular activity was achieved over the initial lead, compound 2.
一系列在稠合苯环的6-和7-位带有增溶侧链的苯胺基(咪唑并喹喔啉)类似物已被制备,并评估了其对Lck酶的抑制作用和对T细胞增殖的抑制作用。与最初的先导化合物2相比,细胞活性有了显著提高。