PMID- 38053851
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20231207
IS  - 2405-8440 (Print)
IS  - 2405-8440 (Electronic)
IS  - 2405-8440 (Linking)
VI  - 9
IP  - 11
DP  - 2023 Nov
TI  - Formation of morpholine-acetamide derivatives as potent anti-tumor drug 
      candidates: Pharmacological evaluation and molecular docking studies.
PG  - e22183
LID - 10.1016/j.heliyon.2023.e22183 [doi]
LID - e22183
AB  - Heterocyclic amines and acetamide derivatives are known for their 
      chemotherapeutic potential. Hence, in the present study, morpholine was taken as 
      a principal product and novel morpholine derivatives were designed, formulated, 
      characterized, and screened for the mechanism of inhibition of carbonic anhydrase 
      and their anticancer potential. In addition, in vitro inhibition of 
      hypoxia-inducible factor-1 (HIF-1) protein was also investigated. Results 
      revealed that compounds 1c, 1d, and 1h possessed significant inhibitory 
      activities against carbonic anhydrase with IC(50) of 8.80, 11.13, and 8.12 muM, 
      respectively. Interestingly, the carbonic anhydrase inhibitory activity of 
      compound 1h was comparable with that of standard acetazolamide (IC(50) 7.51 muM). 
      The compounds 1h and 1i significantly inhibited the proliferation of ovarian 
      cancer cell line ID8 with IC(50) of 9.40, and 11.2 muM, respectively while the 
      standard cisplatin exhibited an IC(50) 8.50 muM. In addition, compounds 1c, 1b, 1h 
      and 1i also exhibited significant inhibitory effects on HIF-1alpha. In conclusion, we 
      report first time the biological potential of morpholine based compounds against 
      ovarian cancer and HIF-1alpha that may serve as lead molecules for drug discovery.
CI  - (c) 2023 The Authors. Published by Elsevier Ltd.
FAU - Sheikh, Ahmed Sadiq
AU  - Sheikh AS
AD  - Department of Pharmaceutical Chemistry, Riphah Institute of Pharmaceutical 
      Sciences, RIU, Islamabad, Pakistan.
FAU - Altaf, Reem
AU  - Altaf R
AD  - Department of Pharmacy, Iqra University, Islamabad, Pakistan.
FAU - Nadeem, Humaira
AU  - Nadeem H
AD  - Department of Pharmaceutical Chemistry, Riphah Institute of Pharmaceutical 
      Sciences, RIU, Islamabad, Pakistan.
FAU - Khan, Muhammad Tariq
AU  - Khan MT
AD  - Faculty of Pharmacy, CUST, Islamabad, Pakistan.
FAU - Murtaza, Babar
AU  - Murtaza B
AD  - Department of Pharmaceutical Chemistry, Riphah Institute of Pharmaceutical 
      Sciences, RIU, Islamabad, Pakistan.
LA  - eng
PT  - Journal Article
DEP - 20231114
PL  - England
TA  - Heliyon
JT  - Heliyon
JID - 101672560
PMC - PMC10694180
OTO - NOTNLM
OT  - Anti-tumor activity
OT  - Carbonic anhydrase inhibition
OT  - HIF-1alpha
OT  - Heterocyclic amines
OT  - MTT (3-[4,5-dimethylthiazole-2-yl]-2,5 diphenyl tetrazolium bromide) assay
OT  - Morpholine based compounds
COIS- The authors have declared no conflict of interest whatsoever.
EDAT- 2023/12/06 06:42
MHDA- 2023/12/06 06:43
PMCR- 2023/11/14
CRDT- 2023/12/06 04:13
PHST- 2023/06/16 00:00 [received]
PHST- 2023/10/31 00:00 [revised]
PHST- 2023/11/06 00:00 [accepted]
PHST- 2023/12/06 06:43 [medline]
PHST- 2023/12/06 06:42 [pubmed]
PHST- 2023/12/06 04:13 [entrez]
PHST- 2023/11/14 00:00 [pmc-release]
AID - S2405-8440(23)09391-X [pii]
AID - e22183 [pii]
AID - 10.1016/j.heliyon.2023.e22183 [doi]
PST - epublish
SO  - Heliyon. 2023 Nov 14;9(11):e22183. doi: 10.1016/j.heliyon.2023.e22183. 
      eCollection 2023 Nov.