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Potentially antibreast cancer enamidines via azide–alkyne–amine coupling and their molecular docking studies

Authors :
Jagannath Jadhav
Prafulla B. Choudhari
Rajashri Salunkhe
Manish S. Bhatia
Rajanikant Kurane
Sharanabasappa Khanapure
Prakash Bansode
Gajanan Rashinkar
Source :
RSC Advances. 6:90597-90606
Publication Year :
2016
Publisher :
Royal Society of Chemistry (RSC), 2016.

Abstract

An attempt to prepare a new triazole series by Cu catalyzed multicomponent reactions of tosyl azide, propargyl bromide and secondary amines led to the synthesis of enamidines. All the synthesized enamidines were evaluated for antiproliferative activities. The four molecules 4a–c and 4h showed higher anticancer activity with GI50 values less than the standard drug doxorubicin against human breast cancer cell line MCF-7. The virtual analysis ascertains the mode of action of these compounds via inhibition of human cell division protein kinase7 (CDK7).

Details

ISSN :
20462069
Volume :
6
Database :
OpenAIRE
Journal :
RSC Advances
Accession number :
edsair.doi...........a7736bcf778d734adc168c25396df6b8