Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3a R ,4 S ,7 R ,7a S )-2-(4-(( E )-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives

Koçyiğit, Ümit Muhammet; BUDAK, YAKUP; GÜRDERE, MELİHA BURCU; Tekin, Şaban; Köprülü, Tuğba Kul; Ertürk, Fatih; Özcan, Kezban; Gülçin, İlhami; CEYLAN, MUSTAFA

doi:10.1016/j.bioorg.2016.12.001

Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3a R ,4 S ,7 R ,7a S )-2-(4-(( E )-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives

Yazarlar (9)

Ümit Muhammet Koçyiğit
Cumhuriyet Üniversitesi, Türkiye

Prof. Dr. Yakup BUDAK Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Prof. Dr. Meliha Burcu GÜRDERE Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Şaban Tekin
Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Tuğba Kul Köprülü
Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Fatih Ertürk
İstanbul Arel Üniversitesi, Türkiye

Kezban Özcan

İlhami Gülçin
Atatürk Üniversitesi, Türkiye

Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Makale Türü	Özgün Makale
Makale Alt Türü	SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı	BIOORGANIC CHEMISTRY
Dergi ISSN	0045-2068 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler	SCI-Expanded
Dergi Grubu	Q4
Makale Dili	İngilizce
Basım Tarihi	02-2017
Cilt No	70
Sayfalar	118 / 125
DOI Numarası	10.1016/j.bioorg.2016.12.001
Makale Linki	http://linkinghub.elsevier.com/retrieve/pii/S0045206816303261

Özet

In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80.51-97.02% compared to 5-FU. Some of the compounds exhibited anti-microbial activity. Also, they evaluated for inhibition effects against human carbonic anhydrase I, and II isoenzymes (hCA I and II) with Ki values in the range of 405.26-635.68pM for hCA I, and 245.40-489.60pM for hCA II, respectively. These results demonstrated that 3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives could be used in different biomedical applications.

Anahtar Kelimeler

BM Sürdürülebilir Kalkınma Amaçları

Atıf Sayıları
WoS	95
Google Scholar	109

Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3a R ,4 S ,7 R ,7a S )-2-(4-(( E )-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives

Dergi Adı	BIOORGANIC CHEMISTRY
Yayıncı	Academic Press Inc.
Açık Erişim	Hayır
ISSN	0045-2068
E-ISSN	1090-2120
CiteScore	8,3
SJR	0,786
SNIP	1,102

Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3a R ,4 S ,7 R ,7a S )-2-(4-(( E )-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives

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