PMID- 24195664
OWN - NLM
STAT- MEDLINE
DCOM- 20141022
LR  - 20211203
IS  - 1875-5607 (Electronic)
IS  - 1389-5575 (Linking)
VI  - 13
IP  - 14
DP  - 2013 Dec
TI  - Recent developments of small molecule PI3K/mTOR dual inhibitors.
PG  - 2047-59
AB  - The phosphoinositide 3-kinases (PI3Ks) are lipid kinases that play a central role 
      in control of cell growth, proliferation, migration, survival and angiogenesis, 
      and drive the progression of tumors by activating phosphoinositidedependent 
      kinase, protein kinase B (Akt) and the mammalian target of rapamycin (mTOR). The 
      PI3K/Akt/mTOR pathway has been shown to play an important role in cancer and has 
      become an important target for anticancer drug development. An interest in 
      targeting two important points along this critical signaling pathway has spurred 
      the development of dual PI3K/mTOR inhibitors that could both prevent cancer cell 
      proliferation and induce programmed cell death (apoptosis) by fully suppressing 
      Akt activation. This review summarizes the developments of a diversity of small 
      molecule dual PI3K/mTOR inhibitors in recent 10 years, with an emphasis on their 
      structural features, the relevant biological activities, and the 
      structure-activity relationships (SARs).
FAU - Liu, Yan-Na
AU  - Liu YN
FAU - Wan, Ren-Zhong
AU  - Wan RZ
FAU - Liu, Zhao-Peng
AU  - Liu ZP
AD  - Department of Organic Chemistry, Key Laboratory of Chemical Biology (Ministry of 
      Education), School of Pharmaceutical Sciences, Shandong University, Jinan 250012, 
      P.R. China. liuzhaop@sdu.edu.cn.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
PL  - Netherlands
TA  - Mini Rev Med Chem
JT  - Mini reviews in medicinal chemistry
JID - 101094212
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Phosphoinositide-3 Kinase Inhibitors)
RN  - 0 (Protein Kinase Inhibitors)
RN  - 0 (Small Molecule Libraries)
RN  - EC 2.7.11.1 (TOR Serine-Threonine Kinases)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/chemistry/pharmacology
MH  - Cell Survival/drug effects
MH  - Humans
MH  - Phosphatidylinositol 3-Kinases/metabolism
MH  - *Phosphoinositide-3 Kinase Inhibitors
MH  - Protein Kinase Inhibitors/*chemistry/pharmacology
MH  - Small Molecule Libraries/*chemistry/pharmacology
MH  - Structure-Activity Relationship
MH  - TOR Serine-Threonine Kinases/*antagonists & inhibitors/metabolism
EDAT- 2013/11/08 06:00
MHDA- 2014/10/23 06:00
CRDT- 2013/11/08 06:00
PHST- 2013/09/05 00:00 [received]
PHST- 2013/10/25 00:00 [revised]
PHST- 2013/10/28 00:00 [accepted]
PHST- 2013/11/08 06:00 [entrez]
PHST- 2013/11/08 06:00 [pubmed]
PHST- 2014/10/23 06:00 [medline]
AID - MRMC-EPUB-57240 [pii]
AID - 10.2174/13895575113136660105 [doi]
PST - ppublish
SO  - Mini Rev Med Chem. 2013 Dec;13(14):2047-59. doi: 10.2174/13895575113136660105.