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

[1] Activation of PI3K/Akt/mTOR Pathway and Dual Inhibitors of PI3K and mTOR in Endometrial Cancer
Chen, Jiezhong
Zhao, Kong-Nan
Li, Rui
Shao, Renfu
Chen, Chen
CURRENT MEDICINAL CHEMISTRY, 2014, 21 (26) : 3070 - 3080
[2] The PI3K/AKT/MTOR signaling pathway: The role of PI3K and AKT inhibitors in breast cancer
Huemer F.
Bartsch R.
Gnant M.
Current Breast Cancer Reports, 2014, 6 (2) : 59 - 70
[3] Status of PI3K/Akt/mTOR Pathway Inhibitors in Lymphoma
Westin, Jason R.
CLINICAL LYMPHOMA MYELOMA & LEUKEMIA, 2014, 14 (05): : 335 - 342
[4] Exploring Novel Therapeutic Targets in GIST: Focus on the PI3K/Akt/mTOR Pathway
Shreyaskumar Patel
Current Oncology Reports, 2013, 15 : 386 - 395
[5] Exploring Novel Therapeutic Targets in GIST: Focus on the PI3K/Akt/mTOR Pathway
Patel, Shreyaskumar
CURRENT ONCOLOGY REPORTS, 2013, 15 (04) : 386 - 395
[6] Evaluation of the PI3K/AKT/mTOR pathway in multiple sclerosis
Mammana, Santa
Fagone, Paolo
Cavalli, Eugenio
Basile, Maria Sofia
Petralia, Maria Cristina
Nicoletti, Ferdinando
Mangano, Katia
INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE, 2017, 40 : S51 - S51
[7] Identification of novel mycocompounds as inhibitors of PI3K/AKT/mTOR pathway against RCC
Yadav, Ravi Prakash
Chatterjee, Srilagna
Chatterjee, Arindam
Pal, Dilip Kumar
Ghosh, Sudakshina
Acharya, Krishnendu
Das, Madhusudan
JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION, 2022, 42 (06) : 599 - 607
[8] Molecular targets for cancer therapy in the PI3K/AKT/mTOR pathway
Polivka, Jiri, Jr.
Janku, Filip
PHARMACOLOGY & THERAPEUTICS, 2014, 142 (02) : 164 - 175
[9] Predictive and pharmacodynamic (PD) markers of PI3K pathway inhibitors: focus on PI3K, AKT and mTOR inhibitors
Tabernero, J.
EUROPEAN JOURNAL OF CANCER, 2011, 47 : S6 - S6
[10] Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors
Welker, Mark E.
Kulik, George
BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 21 (14) : 4063 - 4091

← 1 2 3 4 5 →