On February 10, 2022, Li, Yong; Liu, Yan; Zhu, Zejiang; Yan, Wei; Zhang, Chufeng; Yang, Zhuang; Bai, Peng; Tang, Minghai; Shi, Mingsong; He, Wen; Fu, Suhong; Liu, Jiang; Han, Kai; Li, Jiewen; Xie, Lixin; Ye, Haoyu; Yang, Jianhong; Chen, Lijuan published an article.Electric Literature of 66855-92-3 The title of the article was Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβTubulin Degradation Agents. And the article contained the following:
Compound I, a noncovalent colchicine-site ligand, was capable of promoting αβ-tubulin degradation was found in previous studies. To further improve its antiproliferative activity, derivatives or analogs II [R1 = n-Pr, n-Bu, cyclopentyl, etc.], III [R3 = Et, 2-FC6H4, 3-pyridyl, etc.] of compound I were designed and synthesized based on 2-tubulin cocrystal structure. Among them, compound III [R3 = 1,3-benzodioxol-5-yl] displayed nanomolar potency against a variety of tumor cells, including paclitaxel- and adriamycin-resistant cell lines. Compound III [R3 = 1,3-benzodioxol-5-yl] binds to the colchicine site and promotes αβ-tubulin degradation in a concentration-dependent manner via the ubiquitin-proteasome pathway. The X-ray crystal structure revealed that compound III [R3 = 1,3-benzodioxol-5-yl] binds in a similar manner as compound I, but there was a slight conformation change of the B ring, which resulted in better interaction of compound III [R3 = 1,3-benzodioxol-5-yl] with surrounding residues. Compound III [R3 = 1,3-benzodioxol-5-yl] effectively suppressed tumor growth at an i.v. dose of 40 mg/kg (3 times a week) on both A2780S (paclitaxel-sensitive) and A2780T (paclitaxel-resistant) ovarian xenograft models, with resp. TGIs of 92.42 and 79.75% without obvious side effects, supporting its potential utility as a tumor-therapeutic compound The experimental process involved the reaction of 3-(2-Methoxyphenoxy)benzaldehyde(cas: 66855-92-3).Electric Literature of 66855-92-3
The Article related to amino beta carboline preparation antitumor sar pharmacokinetic human, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 66855-92-3
Referemce:
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Ether | (C2H5)2O – PubChem