Chen, Peng; Zhuang, Yu-Xin; Diao, Peng-Cheng; Yang, Fang; Wu, Shao-Yu; Lv, Lin; You, Wen-Wei; Zhao, Pei-Liang published the artcile< Synthesis, biological evaluation, and molecular docking investigation of 3-amidoindoles as potent tubulin polymerization inhibitors>, Synthetic Route of 38487-85-3, the main research area is amidoindole preparation antiproliferative mol docking tubulin inhibitor human; 3-Amidoindoles; Antiproliferative activity; Microtubules; Tubulin polymerization.
A series of novel 3-amidoindole derivatives possessing 3,4,5-trimethoxylphenyl groups I [R1 = H, Me, Cl, OMe; R2 = 2-thienyl, Ph, 4-FC6H4, etc.] was synthesized and evaluated for their antiproliferative and tubulin polymerization inhibitory activities. Some of them demonstrated moderate to potent activities in vitro against six cancer cell lines including MCF-7, MDA-MB-231, BT549, T47D, MDA-MB-468, and HS578T. The most active compound I [R1 = Cl; R2 = 4-ClC6H4] inhibited the growth of T47D, BT549, and MDA-MB-231 cell lines with IC50 values at 0.04, 3.17, and 6.43 μM, resp. Moreover, the flow cytometric anal. clearly revealed that compound I [R1 = Cl; R2 = 4-ClC6H4] significantly inhibited growth of breast cancer cells through arresting cell cycle in G2/M phase via a concentration-dependent manner. In addition, the compound I [R1 = Cl; R2 = 4-ClC6H4] also exhibited the most potent anti-tubulin activity with IC50 values of 9.5 μM, which was remarkable, compared to CA-4. Furthermore, mol. docking anal. demonstrated the interaction of the compound I [R1 = Cl; R2 = 4-ClC6H4] at the colchicine-binding site of tubulin.
European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Synthetic Route of 38487-85-3.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts