PMID- 25139570
OWN - NLM
STAT- MEDLINE
DCOM- 20150420
LR  - 20211203
IS  - 1464-3405 (Electronic)
IS  - 0960-894X (Linking)
VI  - 24
IP  - 18
DP  - 2014 Sep 15
TI  - Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from 
      a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives.
PG  - 4538-4541
LID - S0960-894X(14)00808-7 [pii]
LID - 10.1016/j.bmcl.2014.07.073 [doi]
AB  - Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of 
      rapamycin (mTOR) signaling pathway by PI3K/mTOR dual inhibitors provides a 
      promising new approach to the treatment of cancers. In this Letter, we identified 
      structurally novel and potent PI3K/mTOR dual inhibitors from a series of 
      2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives. Their synthesis and 
      structure-activity relationships are reported.
CI  - Copyright (c) 2014 Elsevier Ltd. All rights reserved.
FAU - Han, Fangbin
AU  - Han F
AD  - PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life 
      Science Park Road, Changping District, Beijing 102206, PR China.
FAU - Lin, Songwen
AU  - Lin S
AD  - PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life 
      Science Park Road, Changping District, Beijing 102206, PR China.
FAU - Liu, Peng
AU  - Liu P
AD  - PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life 
      Science Park Road, Changping District, Beijing 102206, PR China.
FAU - Tao, Jing
AU  - Tao J
AD  - PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life 
      Science Park Road, Changping District, Beijing 102206, PR China.
FAU - Yi, Chongqin
AU  - Yi C
AD  - PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life 
      Science Park Road, Changping District, Beijing 102206, PR China.
FAU - Xu, Heng
AU  - Xu H
AD  - PKUCare Pharmaceutical R&D Center, A106-109, Biotech Innovation Works, No.29 Life 
      Science Park Road, Changping District, Beijing 102206, PR China. Electronic 
      address: xuheng@pkucare-pharm.com.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20140807
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (2-amino-4-methylpyrido(2,3-d)pyrimidine)
RN  - 0 (Phosphoinositide-3 Kinase Inhibitors)
RN  - 0 (Protein Kinase Inhibitors)
RN  - 0 (Pyrimidines)
RN  - EC 2.7.11.1 (TOR Serine-Threonine Kinases)
SB  - IM
MH  - Crystallography, X-Ray
MH  - Dose-Response Relationship, Drug
MH  - Humans
MH  - Models, Molecular
MH  - Molecular Structure
MH  - Phosphatidylinositol 3-Kinases/metabolism
MH  - *Phosphoinositide-3 Kinase Inhibitors
MH  - Protein Kinase Inhibitors/chemical synthesis/chemistry/*pharmacology
MH  - Pyrimidines/chemical synthesis/chemistry/*pharmacology
MH  - Structure-Activity Relationship
MH  - TOR Serine-Threonine Kinases/*antagonists & inhibitors/metabolism
OTO - NOTNLM
OT  - Anti-tumor activity
OT  - Dual inhibitor
OT  - Mammalian target of rapamycin
OT  - Phosphoinositide 3-kinase
EDAT- 2014/08/21 06:00
MHDA- 2015/04/22 06:00
CRDT- 2014/08/21 06:00
PHST- 2014/05/29 00:00 [received]
PHST- 2014/07/24 00:00 [revised]
PHST- 2014/07/29 00:00 [accepted]
PHST- 2014/08/21 06:00 [entrez]
PHST- 2014/08/21 06:00 [pubmed]
PHST- 2015/04/22 06:00 [medline]
AID - S0960-894X(14)00808-7 [pii]
AID - 10.1016/j.bmcl.2014.07.073 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2014 Sep 15;24(18):4538-4541. doi: 
      10.1016/j.bmcl.2014.07.073. Epub 2014 Aug 7.