Hei, Yuan-Yuan; Zhang, San-Qi; Feng, Yifan; Wang, Jin; Duan, Weiming; Zhang, Hao; Mao, Shuai; Sun, Haopeng; Xin, Minhang published the artcile< Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors>, Reference of 112-63-0, the main research area is alkyl sulfonamide quinazoline derivative preparation oral PI3Ks inhibitor cancer; Anticancer agent; Antiproliferative effects; Drug design; PI3K inhibitor; Quinazoline.
Phosphoinositide 3-kinases (PI3Ks) are regarded as promising targets for treatment of various cancers due to their roles in regulating cell proliferation, differentiation, migration, and survival. Here we report our efforts to develop potent and orally bioavailable PI3K inhibitors for the treatment of cancers. The alkylsulfonamide-containing quinazoline derivatives A1-A18 significantly inhibited PI3Kä¼? and cell proliferation among HCT-116, MCF-7 and SU-DHL-6 cell lines. The optimal compound A1 displayed potent inhibitory activity against PI3Kä¼?(IC50 = 4.5 nM), PI3Kå°?(IC50 = 4.5 nM), PI3Kçº?(IC50 = 4.5 nM), PI3Kæ?(IC50 = 4.5 nM) and significantly inhibited the growth of HCT-116, MCF-7 and SU-DHL-6 cell lines with IC50 values of 0.82æ¸M, 0.99æ¸M and 0.19æ¸M, resp. Western blot anal. demonstrated A1 significantly suppressed the phosphorylation of AKTS473 in a dose-dependent manner. Furthermore, A1 could markedly inhibit cancer growth at the dose of 25 mg/kg in nude mouse HCT-116 xenograft model in vivo without causing significant weight loss or toxicity.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.
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