Synthesis and Evaluation of Cytotoxic Activity of Certain Benzo[h]chromene Derivatives.
Anticancer Agents Med Chem
; 21(8): 963-986, 2021.
Article
in En
| MEDLINE
| ID: mdl-32981512
ABSTRACT
BACKGROUND:
Benzo[h]chromenes attracted great attention because of their widespread biological activities, including anti-proliferate activity, and the discovery of novel effective anti-cancer agents is imperative.OBJECTIVE:
The main objective was to synthesize new benzo[h]chromene derivatives and some reported derivatives, and then test all of them for their anti-cancer activities.METHODS:
The structures of the newly synthesized derivatives were confirmed by elemental and spectral analysis (IR, Mass, 1H-NMR and 13C-NMR). 35 compounds were selected by the National Cancer Institute (NCI) for single-dose testing against 60 cell lines and 3 active compounds were selected for 5-doses testing. Also, these 3 compounds were tested as EGFR-inhibitors; using sorafenib as standard, and as Tubulin polymerization inhibitors using colchicines as a standard drug. Moreover, molecular docking study for the most active derivative on these 2 enzymes was also carried out.RESULTS:
Compounds 1a, 1c and 2b have the highest activities among all 35 tested compounds especially compound 1c.CONCLUSION:
compound 1c has promising anti-cancer activities compared to the used standards and may need further modification and investigations.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Benzopyrans
/
Protein Kinase Inhibitors
/
Tubulin Modulators
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Anticancer Agents Med Chem
Journal subject:
ANTINEOPLASICOS
/
QUIMICA
Year:
2021
Document type:
Article
Affiliation country:
Egypt