PMID- 35114920
OWN - NLM
STAT- MEDLINE
DCOM- 20220916
LR  - 20220923
IS  - 1875-5607 (Electronic)
IS  - 1389-5575 (Linking)
VI  - 22
IP  - 16
DP  - 2022
TI  - Recent Advances in PI3 Kinase Inhibitors: Anticancer Activities and 
      Structure-Activity Relationships.
PG  - 2146-2165
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 the 
      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 the PI3K pathway and/or a specific isoform. The PI3K 
      inhibitors under clinical trial studies include GDC-0032, INK1117 for PI3K-alpha, and 
      AZD8186 for PI3K-beta. This review primarily focuses on the structural insights, 
      anticancer activities, and structure-activity relationship (SARs) 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
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 Isoforms)
RN  - 0 (Quinazolines)
SB  - IM
MH  - *Antineoplastic Agents/pharmacology
MH  - Humans
MH  - Phosphatidylinositol 3-Kinases/metabolism
MH  - *Phosphoinositide-3 Kinase Inhibitors/pharmacology
MH  - Protein Isoforms/metabolism
MH  - Quinazolines
MH  - Structure-Activity Relationship
OTO - NOTNLM
OT  - PI3K
OT  - SAR
OT  - anticancer agents
OT  - kinase
OT  - proliferation
OT  - signaling pathways
EDAT- 2022/02/05 06:00
MHDA- 2022/09/17 06:00
CRDT- 2022/02/04 05:35
PHST- 2021/02/11 00:00 [received]
PHST- 2021/07/27 00:00 [revised]
PHST- 2021/12/01 00:00 [accepted]
PHST- 2022/02/05 06:00 [pubmed]
PHST- 2022/09/17 06:00 [medline]
PHST- 2022/02/04 05:35 [entrez]
AID - MRMC-EPUB-120629 [pii]
AID - 10.2174/1389450123666220202154757 [doi]
PST - ppublish
SO  - Mini Rev Med Chem. 2022;22(16):2146-2165. doi: 10.2174/1389450123666220202154757.