PMID- 36471584
OWN - NLM
STAT- Publisher
LR  - 20240216
IS  - 1875-5607 (Electronic)
IS  - 1389-5575 (Linking)
DP  - 2022 Feb 2
TI  - Recent Advances of PI3 Kinase Inhibitors: Structure Anticancer Activity 
      Relationship Studies.
LID - 10.2174/1389450123666220202154757 [doi]
AB  - Phosphatidyl-inositol-3-kinase (PI3K) has emerged as a potential therapeutic 
      target for the development of novel anticancer drugs. The dysregulation of PI3K 
      has been associated with many human malignancies such as breast, colon, 
      endometrial, brain, and prostate cancers. The PI3K kinases in their different 
      isoforms namely alpha, beta, delta, and gamma, encode PIK3CA, PIK3CB, PIK3CD, and PIK3CG genes. 
      Specific gene mutation or overexpression of the protein is responsible for 
      therapeutic failure of current therapeutics. Recently, various PI3K signaling 
      pathway inhibitors have been identified which showed promising therapeutic 
      results by acting on specific isoforms of the kinase too. Several inhibitors 
      containing medicinally privileged scaffolds like oxadiazole, pyrrolotriazine, 
      quinazoline, quinazolinone, quinazoline-chalcone hybrids, 
      quinazoline-sulfonamide, pyrazolochalcone, quinolone hydroxamic acid, 
      benzofuropyridinone, imidazopyridine, benzoxazines, dibenzoxanthene, 
      indoloderivatives, benzimidazole, and benzothiazine derivatives have been 
      developed to target PI3K pathway and/or a specific isoform. The PI3K inhibitors 
      which are under clinical trial studies include GDC-0032, INK1117 for PI3K-alpha, and 
      AZD8186 for PI3K-beta. This review primarily focuses on the structural insights and 
      structure anticancer activity relationship studies of recent PI3K inhibitors 
      including their clinical stages of development and therapeutic values.
CI  - Copyright(c) Bentham Science Publishers; For any queries, please email at 
      epub@benthamscience.net.
FAU - Asati, Vivek
AU  - Asati V
AD  - Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, 
      India.
FAU - Anant, Arjun
AU  - Anant A
AD  - Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, 
      India.
FAU - Mahapatra, Debarshi Kar
AU  - Mahapatra DK
AD  - Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, 
      Nagpur, Maharashtra, India.
FAU - Bharti, Sanjay Kumar
AU  - Bharti SK
AD  - Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya, Bilaspur, 
      Chhattisgarh, India.
LA  - eng
PT  - Journal Article
DEP - 20220202
PL  - Netherlands
TA  - Mini Rev Med Chem
JT  - Mini reviews in medicinal chemistry
JID - 101094212
SB  - IM
OTO - NOTNLM
OT  - PI3K
OT  - SAR
OT  - anticancer agents
OT  - kinase
OT  - proliferation
OT  - signaling pathways
EDAT- 2022/12/07 06:00
MHDA- 2022/12/07 06:00
CRDT- 2022/12/06 00:53
PHST- 2021/02/11 00:00 [received]
PHST- 2021/07/27 00:00 [revised]
PHST- 2021/12/01 00:00 [accepted]
PHST- 2022/12/06 00:53 [entrez]
PHST- 2022/12/07 06:00 [pubmed]
PHST- 2022/12/07 06:00 [medline]
AID - MRMC-EPUB-120629 [pii]
AID - 10.2174/1389450123666220202154757 [doi]
PST - aheadofprint
SO  - Mini Rev Med Chem. 2022 Feb 2. doi: 10.2174/1389450123666220202154757.