On November 15, 2021, Jie, liu; Ye, Wan; Xu, Jiang-Ping; Wang, Hai-Tao; Li, Xiao-Fang; Wang, Wen-Ya; Zhou, Zhong-Zhen published an article.Category: benzoxazole The title of the article was Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells. And the article contained the following:
To discover PDE4/tubulin dual inhibitors with novel skeleton structures, 7-trimethoxyphenylbenzo[d]oxazoles I [R1 = R2 = H, MeO; R3 = C6H5, 4-MeO-C6H4, 3-F-C6H4, etc] and 4-trimethoxyphenylbenzo[d]oxazoles II [R4 = C6H5, 3,4-MeO-C6H3, 4-F-C6H4, etc] were designed and synthesized by migrating the trimethoxyphenyl group of TH03 to the benzo[d]oxazole moiety. Among these compounds, approx. half of them displayed good antiproliferative activities against glioma (U251) and lung cancer (A549 and H460) cell lines. The structure-activity relationships of trimethoxyphenylbenzo[d]oxazoles led to the identification of I [R1 = H; R2 = MeO; R3 = 1H-indol-5-yl] bearing indol-5-yl side-chain as a novel dual PDE4/tubulin inhibitor, which exhibited satisfactory antiproliferative activities against glioma (IC50 = 300 ± 50 nM) and lung cancer (average IC50 = 39.5 nM) cells. Further investigations revealed that I [R1 = H; R2 = MeO; R3 = 1H-indol-5-yl] induced apoptosis at G2/M phase arrest and disrupted the microtubule network. The preliminary mechanism of action showed that I [R1 = H; R2 = MeO; R3 = 1H-indol-5-yl] down-regulated the expression of cyclin B1 and its upstream regulator gene cdc25C in A549. The experimental process involved the reaction of 7-Bromo-2-phenylbenzo[d]oxazole(cas: 1268137-13-8).Category: benzoxazole
The Article related to trimethoxyphenylbenzoxazole preparation tubulin inhibitor antiproliferative sar, antiproliferative activities, apoptosis, cell cycle arrest, dual pde4/tubulin inhibitor, trimethoxyphenylbenzo[d]oxazole and other aspects.Category: benzoxazole
Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem