Abstract
Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ovarian carcinoma (OVCAR-3) cell lines. Among the 24 synthesized compounds, (2E)-1-(1-(3-morpholinopropyl)-1H-benzimidazol-2 -yl)-3-phenyl-2-propen-1-one) (23a) reduced the proliferation of MCF-7 and OVCAR-3 cell lines demonstrating superior outcomes to those of cisplatin.
| Original language | English |
|---|---|
| Article number | 3259 |
| Journal | Molecules |
| Volume | 24 |
| Issue number | 18 |
| DOIs | |
| Publication status | Published - 2019 Sep 6 |
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All Science Journal Classification (ASJC) codes
- Analytical Chemistry
- Chemistry (miscellaneous)
- Molecular Medicine
- Pharmaceutical Science
- Drug Discovery
- Physical and Theoretical Chemistry
- Organic Chemistry
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Design and synthesis of benzimidazole-chalcone derivatives as potential anticancer agents. / Hsieh, Cheng Ying; Ko, Pi Wen; Chang, Yu Jui; Kapoor, Mohit; Liang, Yu Chuan; Chu, Hsueh Liang; Lin, Hui Hsien; Horng, Jia Cherng; Hsu, Ming-Hua.
In: Molecules, Vol. 24, No. 18, 3259, 06.09.2019.Research output: Contribution to journal › Article
TY - JOUR
T1 - Design and synthesis of benzimidazole-chalcone derivatives as potential anticancer agents
AU - Hsieh, Cheng Ying
AU - Ko, Pi Wen
AU - Chang, Yu Jui
AU - Kapoor, Mohit
AU - Liang, Yu Chuan
AU - Chu, Hsueh Liang
AU - Lin, Hui Hsien
AU - Horng, Jia Cherng
AU - Hsu, Ming-Hua
PY - 2019/9/6
Y1 - 2019/9/6
N2 - Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ovarian carcinoma (OVCAR-3) cell lines. Among the 24 synthesized compounds, (2E)-1-(1-(3-morpholinopropyl)-1H-benzimidazol-2 -yl)-3-phenyl-2-propen-1-one) (23a) reduced the proliferation of MCF-7 and OVCAR-3 cell lines demonstrating superior outcomes to those of cisplatin.
AB - Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ovarian carcinoma (OVCAR-3) cell lines. Among the 24 synthesized compounds, (2E)-1-(1-(3-morpholinopropyl)-1H-benzimidazol-2 -yl)-3-phenyl-2-propen-1-one) (23a) reduced the proliferation of MCF-7 and OVCAR-3 cell lines demonstrating superior outcomes to those of cisplatin.
UR - http://www.scopus.com/inward/record.url?scp=85071936522&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85071936522&partnerID=8YFLogxK
U2 - 10.3390/molecules24183259
DO - 10.3390/molecules24183259
M3 - Article
VL - 24
JO - Molecules
JF - Molecules
SN - 1420-3049
IS - 18
M1 - 3259
ER -