Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway

被引：20

作者：

Lohar, Manoj V. ^{[1
]}

Mundada, Ramswaroop ^{[1
]}

Bhonde, Mandar ^{[2
]}

Padgaonkar, Amol ^{[2
]}

Deore, Vijaykumar ^{[1
]}

Yewalkar, Nilambari ^{[1
]}

Bhatia, Dimple ^{[2
]}

Rathos, Maggie ^{[2
]}

Joshi, Kalpana ^{[2
]}

Vishwakarma, Ram A. ^{[1
]}

Kumar, Sanjay ^{[1
]}

机构：

[1] Nicholas Piramal Res Ctr, Dept Med Chem, Bombay 400063, Maharashtra, India

[2] Nicholas Piramal Res Ctr, Dept Pharmacol, Bombay 400063, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 12期

关键词：

D O I：

10.1016/j.bmcl.2008.04.078

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We herein report the design and synthesis of furoquinoline based novel molecules (16-36) and their in vitro multiple targeted inhibitory potency against PI3K/Akt phosphorylation and mTOR using cell based and cell-free kinase assay. In particular, compound 23 in addition to PI3K-mTOR inhibitory potency, it has shown potent inhibition of hypoxia-induced accumulation of HIF-1 alpha protein in U251-HRE cell line. The inhibitory activities of compound 23 were confirmed by Western blot analysis, using human non-small cell lung carcinoma H-460 cell line and glioblastoma U251 cell lines. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3603 / 3606

页数：4

共 50 条

[21] PI3K/Akt/mTOR Pathway Inhibitors in Cancer: A Perspective on Clinical Progress
Wu, P.
Hu, Y-Z
CURRENT MEDICINAL CHEMISTRY, 2010, 17 (35) : 4326 - 4341
[22] Anti-angiogenic effects of PI3K/Akt/mTOR pathway inhibitors
Friedman, L.
Belvin, M.
Le Couter, J.
Lin, K.
Robillard, L.
Sampath, D.
Stern, H.
Vijapurkar, U.
Ye, W.
Plowman, G.
EJC SUPPLEMENTS, 2008, 6 (12): : 71 - 71
[23] Synthesis, Molecular Docking, In Vitro and In Vivo Studies of Novel Dimorpholinoquinazoline-Based Potential Inhibitors of PI3K/Akt/mTOR Pathway
Zapevalova, Maria, V
Shchegravina, Ekaterina S.
Fonareva, Irina P.
Salnikova, Diana, I
Sorokin, Danila, V
Scherbakov, Alexander M.
Maleev, Alexander A.
Ignatov, Stanislav K.
Grishin, Ivan D.
Kuimov, Alexander N.
Konovalova, Maryia, V
Svirshchevskaya, Elena, V
Fedorov, Alexey Yu
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2022, 23 (18)
[24] PI3K/Akt/mTOR inhibitors in breast cancer
Lee, Joycelyn J. X.
Loh, Kiley
Yap, Yoon-Sim
CANCER BIOLOGY & MEDICINE, 2015, 12 (04) : 342 - 354
[25] PI3K/Akt/mTOR inhibitors in breast cancer
Joycelyn JX Lee
Kiley Loh
Yoon-Sim Yap
Cancer Biology & Medicine, 2015, (04) : 342 - 354
[26] PI3K/AKT/mTOR Inhibitors In Ovarian Cancer
Mazzoletti, M.
Broggini, M.
CURRENT MEDICINAL CHEMISTRY, 2010, 17 (36) : 4433 - 4447
[27] PI3K/Akt/mTOR inhibitors in breast cancer
Joycelyn JX Lee
Kiley Loh
Yoon-Sim Yap
Cancer Biology & Medicine, 2015, 12 (04) : 342 - 354
[28] Synthesis and Biological Activity of Novel PI3K/mTOR Inhibitors
Wang Lei
Zheng Guojun
Ji Qi
Chen Bo
Gong Longlong
Gao Congmin
Du Zhenjian
Zhang Xingmin
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2017, 38 (09): : 1590 - 1595
[29] RAS Signaling in the PI3K/AKT/MTOR Pathway
Nussinov, Ruth
Zhang, Mingzhen
Jang, Hyunbum
BIOPHYSICAL JOURNAL, 2020, 118 (03) : 51A - 51A
[30] PI3K-AKT-mTOR pathway inhibitors
Cortot, A
Armand, JP
Soria, JC
BULLETIN DU CANCER, 2006, 93 (01) : 19 - 26

← 1 2 3 4 5 →